TW200811112A - Benzimidazole derivatives - Google Patents

Abstract

The invention is concerned with novel benzimidazole derivatives of formula (I), wherein R1 to R8 are as defined in the description and in the claims, as well as physiologically acceptable salts and esters thereof. These compounds bind to FXR and can be used as medicaments.

Description

200811112 IX. Description of the invention: [Technical field to which the invention pertains] The present invention relates to novel benzimidazole derivatives of formula (I) r1\

Wherein R is Cl-l decyl, lower alkoxy-lower alkyl, lower alkoxy-carbonyl-lower alkyl, cycloalkyl, cycloalkyl-lower alkyl, aryl, Aryl-lower alkyl, di-aryl-lower alkyl, heteroaryl, heteroaryl-lower alkyl, heterocyclyl or heterocyclyl-lower alkyl, wherein cycloalkyl, aryl The base, heteroaryl or heterocyclic group is optionally substituted by 1 to 3 substituents independently selected from the group consisting of lower alkyl, lower alkoxy, lower alkoxy- Carbonyl, morpholinyl, formamidine, halogen, hydroxy, fluoro-lower alkyl, fluoro-lower alkoxy, lower alkyl-carbonyl-N (lower alkyl), lower alkyl- Carbonyl-N(H), NH2, N(H, lower alkyl), N(lower alkyl)2, carboxyl, aminemethanyl, N(H, lower alkyl)C(O) and N (lower alkyl) 2C(0); R2 is hydrogen or lower alkyl; R is lower carbon, calcined, partially unsaturated, aryl, square 121967.doc 200811112 base-low carbon Alkyl, heteroaryl, heteroaryl-lower alkyl, heterocyclic or heterocyclic; lower alkyl, wherein aryl, heteroaryl or heterocyclic Substituting 1 to 3 substituents independently selected from the group consisting of halogen, lower alkyl, lower alkoxy, lower alkoxy-carbonyl, hydroxy, fluoro-low Carboalkyl, fluoro-lower alkoxy, NH2, N(H, lower alkyl), N (lower alkyl) 2, lower alkyl-carbonyl-N (lower alkyl), low carbon Alkyl-carbonyl-hydrazine), carboxyl group, amine carbenyl group, N(H, lower alkyl)C(O) and N(lower alkyl) 2C(0); R4 is a) as the case may be 1 to 3 heteroaryl groups independently selected from the group consisting of lower alkyl, phenyl, lower alkoxy-carbonyl, carboxyl, aminecaraki, N (H, low carbon) Alkyl)C(O), N(lower alkyl)2C(0), NH2, N(H, lower alkyl), N(lower alkyl)2, lower alkyl-carbonyl-N ( Lower alkyl), lower alkyl-carbonyl-N(H), hydroxy, lower alkoxy, halogen, fluoro-lower alkyl, fluoro-low oxime alkoxy, nitrogen and hydrazin; b) unsubstituted naphthyl or naphthyl or phenyl substituted with 1 to 3 substituents independently selected from the group consisting of halogen, hydroxy, NH2 , CN, hydroxy-lower alkyl, lower alkoxy, lower alkyl-carbonyl, lower alkyl-carbonyl-N(H), lower alkoxy-carbonyl, aminoxime, di- Lower alkyl-amine sulfonyl, lower alkyl-sulfonyl, thienyl, pyrazolyl, thiadiazolyl, imidazolyl, triazolyl, tetrazolyl, 2-sided oxy-tonol Sulfhydryl, ° thiol, sulfhydryl, sulfhydryl, 121967.doc 200811112 2 - pendant oxy-pyrazine, σ piroxime, slightly fluorenyl, oxime, 嗟n, Oxadiazolyl, carboxyl, lower alkyl, fluoro-lower alkyl, fluoro-lower alkoxy, N(H, lower alkyl), N (lower alkyl) 2, lower alkyl -carbonyl-N (lower alkyl), amine sulfhydryl, N (H, lower alkyl) C(O), N (lower alkyl) 2C (0), lower alkyl-amine sulfonium a phenyl group, a phenyloxy group, a phenoxy group, and optionally a phenyl group substituted with one or three substituents independently selected from the group consisting of a nucleus and a fluoro-lower alkyl group; or c) if R3 is a cycloalkyl group, R4 is a cycloalkyl group, and R4 is also a phenyl group; R5, R6, R7 and R8 are each independently an anthracene, a _ or a lower alkyl group, or R5 and R are bonded together, Or R6 and R7 are bonded together, or R7 and R8 are bonded together, together with the carbon atom to which they are attached, form a 7-membered aromatic or non-aromatic carbocyclic or heterocyclic ring; and pharmaceutically acceptable Salts and esters; wherein the compound of formula (I) is not selected from the group consisting of 2-[2-(2-a-phenyl)-benzimidazole-indenyl]methyl-pentanoic acid Butyl decylamine and 2-(2-benzo[1,3]dioxol-5-yl-benzimidazole-indenylbenzyl-butanamine. Further, the present invention relates to a method for producing the above compound, a w drug preparation containing the same, and the use of the same for the manufacture of a pharmaceutical preparation. [Prior Art] Farnesoid X-like body (Farnes〇id_x_recept〇r (FxR) is a nuclear factor receptor superfamily of transcription factors that is υνϋ^. FXR was originally identified as being the main source of bile acid receptors by farnesol/fork_'subsequent research*FXR 121967.doc 200811112

To be effective [Makishima, M., Okamoto, A. Y., Repa, J. J., Tu, H., Learned, RM, Luk, A., Hull, Μ. V., Lustig, K. D., Mangelsdorf, D. J. and Shan, B. (1999) Identification of a nuclear receptor for bile acids. Science 284, 1362-5] o FXR is expressed in the liver, intestine, kidney and adrenal glands. Four splicing isoforms have been cloned in humans. Among the major bile acids, chodeoxycholic acid is the most effective FXR agonist. Binding of bile acids or synthetic ligands to FXR induces a small heterodimer partner (SHP), a member of the atypical nuclear receptor family that binds to several other nuclear hormone receptors (including LRH-1) And LXRa) transcriptional expression, and block its transcriptional function [Lu, T. T., Makishima, M., Repa, J. J., Schoonjans, K., Kerr, Τ·A., Auwerx, J. and Mangelsdorf, DJ (2000) Molecular basis for feedback regulation of bile acid synthesis by nuclear receptors· Mol Cell 6, 507-15]. CYP7A1 and CYP8B are enzymes involved in the synthesis of hepatobiliary acid. FXR inhibits its performance by activating the SHP pathway. FXR directly induces the expression of the bile acid export transporter of the ABC family in hepatocytes. These transporters include the bile salt export pump (ABCB 11) and the multidrug resistance associated protein 2 (multidrug resistance associated protein). 2) (ABCC2) [Kast, H. R., Goodwin, B., Tarr, P. T., Jones, S. A., Anisfeld, A. M., Stoltz, C. M., Tontonoz, P· , Kliewer, S., Willson, Τ·M· and Edwards, PA (2002) Regulation of multidrug resistance-associated protein 2 (ABCC2) by the nuclear receptors 121967.doc -10- 200811112 pregnane X receptor, farnesoid X-activated receptor , and constitutive androstane receptor. J Biol Chem 277, 2908-15 ; Ananthanarayanan, M·, Balasubramanian, N·,

Makishima, M., Mangelsdorf, D. J. and Suchy, F. J. (2001) Human bile salt export pump promoter is transactivated by the farnesoid X receptor/bile acid receptor. J Biol Chem 276, 28857-65]. FXR knockout mice have reduced resistance to bile acid-induced hepatic poisoning and have demonstrated that synthetic FXR agonists are hepatoprotective in animal models of cholestasis [Liu, Y., Binz, J., Numerick, MJ, Dennis , S·, Luo, G·, Desai, B·, MacKenzie, Κ· I., Mansfield, Τ· A., Kliewer, SA, Goodwin, B. and Jones, SA (2003) Hepatoprotection by the farnesoid X receptor agonist GW4064 in rat models of intra- and extrahepatic cholestasis· J Clin Invest 112,1678-87 ; Sinal, C. J., Tohkin, M·, Miyata, M·, Ward, J. M·, Lambert, G· and Gonzalez , FJ (2000) Targeted disruption of the nuclear receptor FXR/BAR impairs bile acid and lipid homeostasis. Cell 102, 731-44]. These data show that FXR protects liver cells from bile acid toxicity by inhibiting cell synthesis and bile acid input and by stimulating their bile secretion. The process of bile acid enterohepatic circulation is also a major regulator of serum cholesterol homeostasis. After biosynthesis from cholesterol in the liver, bile acids are secreted together with bile in the lumen of the small intestine to aid in the digestion and absorption of fat and fat-soluble vitamins. The ratio of different bile acids determines the hydrophilicity of the bile acid pool and its ability to dissolve cholesterol in 121967.doc -11- 200811112. FXR activation increases the hydrophilicity of the pool, reduces the intestinal solubility of cholesterol, and effectively blocks its absorption. It would be desirable to reduce absorption resulting in a decrease in plasma cholesterol levels. In fact, direct inhibitors of cholesterol absorption, such as ezetimibe, lower plasma cholesterol, which provides some evidence to support this hypothesis. However, ezetimibe has a limited effect, which is attributed to the feedback of cholesterol synthesis in the cells. Up regulation attempts to compensate for the loss of cholesterol. Recent data have shown that FXR partially has this effect by directly inhibiting the performance of HMGCoA reductase via pathways involving SHP and LRH1 [Datta, S., Wang, L., Moore, DD and Osborne, TF (2006) Regulation of 3 -hydroxy-3-methylglutaryl coenzyme A reductase promoter by nuclear receptors liver receptor homologue-1 and small heterodimer partner: a mechanism for differential regulation of cholesterol synthesis and uptake. J Biol Chem 281,807-l2]. FXR also reduces hepatic synthesis of triglycerides by inhibiting SREBP1-c expression by alternative pathways involving SHP and LXRcx. Thus, compounds that modulate FXR activity can exhibit superior therapeutic efficacy for plasma cholesterol and triglycerides to a greater extent than current therapies. Most patients with coronary heart disease have a high plasma content of atherogenic LDL. The HMGCoA reductase inhibitor (statin) is effective in normalizing LDL-C levels, but only reduces the risk of cardiovascular events such as stroke and myocardial infarction by approximately 30%. There is a need for other therapies that further reduce atherogenic LDL and other lipid risk factors such as high plasma triglyceride levels and low HDL-C levels. 121967.doc -12- 200811112 In the United States, a high proportion of patients with type 2 diabetes have abnormal plasma lipoprotein concentrations. The incidence of total cholesterol >24〇mg/dii was 37% in male diabetic patients and 44% and 1^1^ in female diabetic patients (:>16〇111§/(the incidence rate of 11 Among the populations, 31% and 44% respectively. Diabetes is a disease in which the ability of patients to control the blood glucose level is reduced due to partial loss of the response to Tengdaosu. In developed countries, π-type diabetes (T2D) is also It is called non-insulin-dependent diabetes mellitus (NIDDM), which accounts for 80-90% of all cases of diabetes. In T2D, the pancreatic islets of Langerhans produce insulin but the main target tissues (muscle, liver and adipose tissue) It is extremely resistant to its effects. The body supplements 4 shells by producing more insulin, which ultimately leads to impaired insulin production in the pancreas. Therefore, T2D is a cardiovascular metabolic syndrome associated with com〇rbidity. These comorbidities include dyslipidemia and insulin resistance as well as hypertension, endothelial dysfuncti〇n and inflammatory atherosclerosis. Dyslipidemia and diabetes First-line treatment is low-fat and low-glucose drinking, exercise, and weight loss. Compliance can be necessary for the treatment of moderate and developed metabolic defects such as, for example, statins and fibric acid Lipid regulators, hypoglycemic agents such as sulfonyl urea and metformin, or insulin sensitizers of the terpene dione (TZD) class of ρρΑΚγ agonists. Recent studies provide evidence for FXR modulators The high normalization of kt, DL C and glycerol/diacetate content may have enhanced therapeutic potential and is currently only achieved in combination with existing drugs and, in addition, may avoid feedback effects on cellular cholesterol homeostasis. 121967.doc - 13- 200811112 The novel compounds of the present invention are superior to the compounds known in the art because they bind FXR very efficiently and selectively modulate fxr. Therefore, lowering cholesterol absorption, lowering LDL cholesterol and triglycerides and reducing inflammatoryness Atherosclerosis. Because multiple aspects of combined dyslipidemia and cholesterol homeostasis are addressed by FXR modulators, it is expected FXR modulators have enhanced therapeutic potential compared to compounds already known in the art. [Description] Unless otherwise indicated, the following definitions are set forth to illustrate and define the various terms used herein to describe the invention. Meaning and scope. In the present specification, the term "low carbon," is used to mean a group consisting of 1 to 7, preferably 1 to 4 carbon atoms. The term "halogen" means fluorine, chlorine, Bromine and iodine, wherein fluorine, gas and bromine are preferred. The term "alkyl", alone or in combination with other groups, means 1 to 2 carbon atoms, preferably 1 to 16 carbon atoms, more preferably 1 to 1. A branched or linear monovalent saturated aliphatic hydrocarbon group of one carbon atom. Lower alkyl groups as described below are also preferred alkyl groups. The term "C^oalkyl" refers to a branched or straight-chain monovalent saturated aliphatic hydrocarbon group of from i to 1 carbon atoms, such as methyl, ethyl, n-propyl, isopropyl, n-butyl, a second butyl group, a tert-butyl group, a pentyl group, a tetramethyl-butyl group, and the like. The "low sulphonyl group" alone or in combination with other groups means 1 to 7 carbon atoms. A branched or linear monovalent alkyl group of 1 to 4 carbon atoms. The term is further exemplified by groups such as methyl, ethyl, n-propyl, isopropyl, n-butyl, t-butyl, t-butyl and the like. 121967.doc • 14 - 200811112 Mission. The lower alkyl group may optionally be substituted with, for example, a hydroxyl group. These substituted lower alkyl groups are referred to as π hydroxy-lower alkyl groups. Unsubstituted lower alkyl groups are preferred. The term ''fluoro-lower alkyl' refers to a lower alkyl group which is mono- or polysubstituted by fluorine. Examples of fluorine-low carbon alkyl groups are, for example, CFH2, cf2h, cf3, CF3CH2, CF3(CH2)2. (CF3) 2CH and CF2H-CF2. The term ''amino group' alone or in combination means that a primary, primary or secondary amine group is bonded via a nitrogen atom, wherein the secondary amine group carries a monoalkyl or cycloalkyl substituent And the secondary amine group carries two similar or different alkyl or cycloalkyl substituents or the two nitrogen substituents together form a ring, such as ΝΗ2, methylamino, ethylamino, dimethylamino , diethylamino group, methyl-ethylamino group, pyrrolidin-1-yl or fluorenyl-piperidinyl group, etc., preferably a primary amino group, a dimethylamino group and a diethylamino group and especially Dimethylamino group. The term "mercaptoamine" refers to the group HC(0)-N(H)-. The term "cycloalkyl" refers to a monovalent carbocyclic group of 3 to 10 carbon atoms, preferably 3 to 6 carbon atoms, such as cyclopropyl, cyclobutyl, cyclopentyl or cyclohexyl. The cycloalkyl group can be optionally substituted as described in the examples and the scope of the patent application. The term "partially unsaturated cycloalkyl" refers to a monovalent carbocyclic group having from 3 to 1 carbon atoms, preferably from 4 to 8 carbon atoms, having from 4 to 4 double bonds, such as cyclohexenyl, cyclopentane. Alkenyl, cycloheptadienyl. The term 'alkoxy' refers to the group R, 〇 〇, where R is an alkyl group. The term "low carbon alkoxy" refers to the group R, 〇 〇, where R is a lower alkane. base. The term ''fluoro-lower alkoxy group' refers to the group RM_〇_, where R, is a fluorine-low 121967.doc -15- 200811112 stone anti-burning group. An example of a fluorine-lower alkoxy group is (for example) CFh2_〇, CF2li_〇, cf3-〇, Cf3CH2 〇, CF3(CH2)2_〇, (CF3)2CH_〇, and CF2H-CF2-〇〇 垂 n aryl) benzene alone or in combination Or a naphthyl group, preferably a phenyl group, which may optionally be substituted with from 1 to 5, preferably from 1 to 3, substituents independently selected from the group consisting of lower alkyl, lower alkoxy , halogen, hydroxy, CN, CF3, amine, aminocarbonyl, carboxyl, N〇2, lower alkyl acid group, aminosulfonyl, lower alkylcarbonyl, lower alkylcarbonyloxy, Lower alkylcarbonyl-N(H), lower alkyl-carbonyl-N (lower alkyl), lower alkoxycarbonyl, fluoro-lower alkyl, fluoro-lower alkoxy, naphthenic Base, phenoxy', methyl-oxadiazolyl, morphinyl, decylamino. Preferred substituents are i-, lower alkyl, fluoro-lower alkyl and CN. Further, the aryl group is preferably substituted as described in the following embodiments and patent applications. The term "heteroaryl" refers to an aromatic 5 to 6 membered monocyclic ring or a 9 to 10 membered bicyclic ring which may contain 1, 2 or 3 atoms selected from nitrogen, oxygen and/or sulfur, such as furyl, σ-pyridyl. Base, 2-sided oxy-1,2-dihydro-pyridyl, pyridazinyl, pyrimidinyl, 17-indenyl, porphinyl, iso-t-seat, sigma-based. Oxadisyl, tertyl, pyrrolyl, pyrazolyl, triazolyl, tetrazolyl, thiazolyl, isothiophene, 1,2,3-thiadiazolyl, benzodioxole Alkenyl, benzoidenyl, fluorenyl, isodecyl, 1,3-dihydroxy-isoindolyl, quinolinyl, oxazolyl, benzisothiazolyl, benzoxazole Base, benzoisoindenyl, benzoquinone, benzoxepylene, benzofuranyl and oxime. Preferred heteroaryl groups are pyridyl, pyrimidinyl, oxazolyl, benzodioxolanyl, porphinyl, σ-haha, 2-oxax-1,2-dihydro-σ ratio Bite base, 121967.doc -16 - 200811112 ° σ 朵 基 喑, 喑 臭 、, 吩 吩 、, 笨 噢 四 四 四 四 四 四 四 四 四 四 四 四 四 四 四 四 四 四 四 卩 、 、 、 、 、 、 、 、 、 r /, benzocylate, sulphate, sulphate, sulphate, aryl, aryl, aryl, aryl, aryl, aryl, aryl, aryl, aryl, aryl, aryl Preferably, it can be as described in the following paragraph. The term "heterocyclic group," means 5 to 6 members of the atomic group. W selects ", oxygen and/or sulfur, thiophene. Morpholine shellfish or tricyclic, such as morpholinium, ^ ^, an oxy-thiamorpholinyl, piperidinyl, 2-sided oxygen storm - mouth-based base, mouth blowing 8 oxygen... side oxygen Base·deuterium (tetra)yl, ...-keto, bicyclo[...]octyl, phenylzinyl and tetrahydro bromo. The silk is a W group, a 2-side oxygen-containing filament, a feed bite group, a 2-side 1 group/bite group, and a tetrahydro group. The heterocyclic group may optionally have the aforementioned "holding" associated with the term "aryl". Further, the heterocyclic group is preferably substituted as described in the following Becker and K.S. patents. U stays 4 bases' refers to groups which are used to temporarily protect functional groups, especially via groups. Examples of protecting groups are benzyl, p-methoxyphenyl fluorenyl, tert-butylmethyl sulphate, t-butyl-diphenyl sulphate, and (for protecting amine groups) Boc and benzyloxy Alkylcarbonyl. The compound of formula (I) forms a pharmaceutically acceptable acid addition salt. Examples of such pharmaceutically acceptable salts are those formed by the compound of formula (1) with a physiologically compatible inorganic acid such as hydrochloric acid, sulfuric acid, sulfurous acid or phosphoric acid, or a salt formed with an organic acid. Such organic acids are, for example, methanesulfonic acid, p-toluenesulfonic acid, acetic acid, lactic acid, trifluoroacetic acid, citric acid, fumaric acid, maleic acid, tartaric acid, succinic acid or salicylic acid. The term "medicine 121967.doc -17- 200811112 "studently acceptable salt" refers to such salts. The compound of the formula (1) in which a C〇OH group is present may further form a salt with a base. Examples of such salts are alkali metal salts, alkaline earth metal salts and phosphonium salts such as sodium, potassium, calcium and trimethylammonium salts. The term π pharmaceutically acceptable salt also refers to such salts. Salts obtained by the addition of an acid are preferred. The term ''pharmaceutically acceptable esters" includes derivatives of the compounds of formula (1), wherein treason Already converted to esters. Lower alkyl, hydroxy-lower alkyl, lower carbon oxy-lower alkyl, amine _ lower alkyl, mono or di-lower alkyl-amino-low carbon Anthracenyl, oxime-morpholinyl-lower alkyl, Ν-pyrrolidinyl-lower alkyl, oxime-bunkenyl-lower alkyl, Ν-piperazinyl-lower alkyl, lower alkane The base Ν-Ν-carbazinyl-lower alkyl and aralkyl esters are examples of suitable esters. Methyl, ethyl, propyl, butyl and benzyl esters are preferred esters. Methyl esters and ethyl esters Esters are especially preferred. The term "pharmaceutically acceptable esters", in addition to the compounds of the formula (I) wherein the mesogenic groups have been converted to the corresponding esters with inorganic or organic acids which are not toxic to the biological organism, such acids , sulfuric acid, phosphoric acid, citric acid, formic acid, maleic acid, acetic acid, succinic acid, tartaric acid, methanesulfonic acid, p-toluene acid and the like. DETAILED DESCRIPTION OF THE INVENTION The present invention relates to compounds of formula (I)

121967.doc -18- 200811112 wherein R is Ci, alkyl, lower alkoxy-lower alkyl, lower alkoxy-carbonyl-lower alkyl, cycloalkyl, cycloalkyl-lower alkane Alkyl, aryl, aryl-lower alkyl, di-aryl-lower alkyl, heteroaryl, heteroaryl-lower alkyl, heterocyclyl or heterocyclyl-lower alkyl, wherein The cycloalkyl, aryl, heteroaryl or heterocyclic group is optionally substituted with 3 substituents independently selected from the group consisting of lower alkyl, lower alkoxy, lower carbon Alkoxy-carbonyl, morpholinyl, formamide, hydroxy, fluoro-lower alkyl, fluoro-lower alkoxy, lower alkyl-carbonyl-N (lower alkyl), Lower alkyl _ carbonyl _ N (H), NH 2 , N (H, lower alkyl), n (lower alkyl) 2, carboxyl, amine sulfhydryl, N (H, lower alkyl) C (O) and N (lower alkyl) 2. (0); R2 is hydrogen or lower alkyl; R3 is lower alkyl, cycloalkyl, partially unsaturated ring, aryl, aryl-lower alkyl, heteroaryl, heteroaryl- a lower alkyl group, a heterocyclic group or a heterocyclic group-lower alkyl group, wherein the aryl group, heteroaryl group or heterocyclic group is optionally one to three substituents independently selected from the group consisting of the following groups; Substituted: halogen, low carbon yard, low carbon alkoxy, low carbon alkoxy-based, light, gas-lower alkyl, fluorine-lower alkoxy, NH2, N (H, low carbon Alkyl), N (lower alkyl) 2, lower alkyl-carbonyl-N (lower alkyl), lower alkyl-carbonyl-N(H), carboxyl, amine sulfhydryl, N (H) , lower alkyl) C(O) and N(lower alkyl) 2C(0); 121967.doc -19- 200811112 R4 is a) optionally 1 to 3 independently selected from the following groups a heteroaryl group substituted with a substituent of a group: lower alkyl, phenyl, lower alkoxy-carbonyl, carboxy, aminecarbamyl, N(H, lower alkyl)C(O), N (low Carboalkyl) 2C(0), NH2, N(H, lower alkyl), N(lower alkyl) 2, lower alkyl-carbonyl-N (lower alkyl), lower alkane -carbonyl-N(H), hydroxy, lower alkoxy, halogen, fluoro-lower alkyl, fluoro-lower alkoxy, cyano and morpholinyl; b) unsubstituted naphthyl, Or a naphthyl or phenyl group substituted with 1 to 3 substituents independently selected from the group consisting of halogen, trans-group, NH2, CN, hydroxy-lower alkyl, lower alkoxy, lower Carboalkyl-carbonyl, lower alkyl-carbonyl-N(H), lower alkoxy-carbonyl, aminsulfonyl, di-lower alkyl-amine sulfonyl, lower alkyl-sulfonate Base, phenyl group, ton sulphate, sulfonium sulfonate, miso base, triterpene group, tetra-l-based group, 2-sided oxy-indolyl thiol base, σ-pyramid, ° ratio bite base, mouth σ定基, 2-o-oxy-tung, 吼L base, brigade base, ° σ 坐 sit, σ σ sit, σ 恶 二 U sit, rebel, low carbon burn, gas - lower alkyl, fluoro-lower alkoxy, hydrazine (hydrazine, lower alkyl), hydrazine (lower alkyl) 2, lower alkyl-carbonyl-hydrazine (lower alkyl), amine Sulfhydryl, hydrazine (hydrazine, lower alkyl) c(0), hydrazine (lower alkyl) 2C (0), lower alkyl-amine sulfonyl, lower alkenyl, benzhydryl, An oxy group and optionally a phenyl group substituted with one or three substituents independently selected from the group consisting of halogen and a fluoro-lower alkyl group; or c) if R3 is a cycloalkyl group, R4 is a cycloalkyl group, and R4 may also be Is phenyl; 121967.doc -20· 200811112 R / and R are each independently H, i or low carbon, or R5 and 6 are combined, or R6 and R7 are combined, or R7 and R are bonded to form a 4-7 membered aromatic or non-aromatic carbocyclic or heterocyclic ring together with the carbon atom to which they are attached; and pharmaceutically acceptable salts and esters thereof; The compound of formula (I) is not selected from the group consisting of 2-[2-(2-chloro-phenyl)-benzimidazole "- keb #•methyl-pentanoic acid butyl decylamine and 2 ( 2-Bisto[1,3]dioxol-5-yl-benzimidazole_丨_yl)_N_benzyl_butanamine. In the compound of the formula (1) as described above, preferably, R4 is a) a heteroaryl group optionally substituted with 1 to 3 substituents independently selected from the group consisting of lower alkyl groups, Phenyl, lower alkoxy-carbonyl, carboxyl, aminemethanyl, N(H, lower alkyl) C(〇), N(lower alkyl) 2C(0), NH2, N(H, Lower alkyl), N (lower alkyl) 2, lower alkyl-carbonyl-N (lower alkyl), lower alkyl-carbonyl-n(H), hydroxy, lower alkoxy, a dentin, a fluorine-low carbon alkyl group and a fluorine-low carbon alkoxy group; b) an unsubstituted naphthyl group or a naphthyl group substituted with 1 to 3 substituents independently selected from the group consisting of the following groups or Phenyl group: halogen, hydroxy, NH2, CN, hydroxy-lower alkyl, lower alkoxy, lower alkyl-carbonyl, lower alkyl-carbonyl-N(H), lower alkoxy-carbonyl Acesulfonyl, di-lower alkyl-amine sulfonyl, lower alkyl-sulfonyl, thienyl, pyrazolyl, thiadiazolyl, imidazolyl, triazolyl, tetrazolyl, 2-sided oxy-pyrrolidinyl group, ° ratio σ group, 咕σ group, mouth σ group, 2-sided oxy-bite group, 吼Olefin, piperidinyl, oxazolyl, thiazolyl, oxadiazolyl, carboxy, lower alkyl, 121967.doc -21- 200811112 fluoro-lower alkyl, fluoro-lower alkoxy, N ( H, lower alkyl), N (lower alkyl) 2, lower alkyl-carbonyl-N (lower alkyl), amine fluorenyl, N(H, lower alkyl) C(O) And N (lower alkyl) 2C (0) and lower alkyl-amine sulfonyl; or C) if R 3 is a cycloalkyl, R 4 is a cycloalkyl group, and R 4 may also be a phenyl group. These compounds are characterized by formula (I)

Vr2

Wherein R is a C 1 _ 1 Q alkyl group, a low carbon alkoxy group - a low carbon alkyl group, a low carbon alkoxy group - a rotam group - a lower alkyl group, a cycloalkyl group, a cycloalkyl group or a lower alkyl group, Aryl, aryl-lower alkyl, di-aryl-lower alkyl, heteroaryl, heteroaryl-lower alkyl, heterocyclyl or heterocyclyl-lower alkyl, wherein cycloalkane The aryl group, the aryl group, the heteroaryl group or the heterocyclic group are optionally substituted by 1 to 3 substituents independently selected from the group consisting of low sulfoalkyl groups, low carbon alkoxy groups, and low carbon burns. Oxy-Wilyl, morphinyl, formamidine, halogen, hydroxy, fluoro-lower alkyl, fluoro-lower alkoxy, lower alkyl-carbonyl-N (lower alkyl), low Carboalkyl-carbonyl_N(H), NH2, N(H, lower alkyl), N(lower alkyl)2, 鲮121967.doc -22- 200811112, amidino, N(H , lower alkyl) c (〇) and N (lower alkyl) 2C (0); R is hydrogen or low carbon alkyl; R is a low carbon alkyl, cycloalkyl, partially unsaturated cycloalkyl, Aryl, aryl-lower alkyl, heteroaryl, heteroaryl-lower alkyl, heterocyclyl or heterocyclyl-lower alkyl, wherein aryl, heteroaryl or The ring group is optionally substituted with from 1 to 3 substituents independently selected from the group consisting of: _, lower alkyl, lower alkoxy, lower alkoxy-alkyl, thiol , fluorine-low carbon alkyl, fluorine-low carbon alkoxy, NH2, N (H, lower alkyl), N (lower alkyl) 2, lower alkyl-carbonyl-N (lower alkyl) ), lower alkyl-carbonyl-N(H), carboxyl, amine fluorenyl, N(H, lower alkyl)C(O) and N(lower alkyl) 2C(0); R4 is a a heteroaryl group optionally substituted with one or three substituents selected from the group consisting of a lower alkyl group, a phenyl group, a lower alkoxy group-carbonyl group, a carboxyl group, an amine methyl group, N (H, lower alkyl) C (O), N (lower alkyl) 2C (0), NH2, N (H, lower alkyl), N (lower alkyl) 2, lower alkane alkyl-carbonyl-N (lower alkyl), lower alkyl-carbonyl-N(H), thiol, lower alkoxy, halogen, fluoro-lower alkyl and fluoro-lower alkoxy; b) unsubstituted naphthyl, or naphthyl or phenyl substituted with 1 to 3 substituents independently selected from the group consisting of halogen, hydroxy, NH2, CN, thiol - low carbon alkyl, low carbon alkoxy, lower alkylcarbonyl, lower alkyl-carbonyl-N(H), lower alkoxy-carbonyl 121967.doc -23- 200811112 base, amine sulfonyl , bis-lower alkyl-amine sulfonyl, lower alkyl-sulfonyl, U-secenyl, σ-mercapto, indenyl, indolyl, tris-s, tetrazolyl, 2 - pendant oxy-pyrrolidinyl, pyrrolyl, pyridyl, . Bite, 2-oxo-piperidinyl, pyrrolidinyl, piperidinyl, oxazolyl, oxazolyl, oxadiazolyl, carboxyl, lower alkyl, fluoro-low carbon alkyl - lower alkoxy, hydrazine (hydrazine, lower alkyl), hydrazine (lower alkyl) 2, lower alkyl-carbonyl-hydrazine (lower alkyl), amine indenyl, hydrazine (hydrazine, Lower alkyl)C(O), fluorene (lower alkyl) 2C(0) and lower alkyl-amine sulfonyl; or C) if R3 is cycloalkyl, then R4 is cycloalkyl, R4 It may also be a phenyl group; R, R, R7 and R8 are each independently an anthracene, a halogen or a lower alkyl group, or a combination of R5 and a chemical system, or a combination of R6 and R7, or a combination of R7 and R Together, together with the carbon atom to which they are attached, form a 4-7 membered aromatic or non-aromatic carbocyclic or heterocyclic ring; and pharmaceutically acceptable salts and esters thereof; wherein the compound of formula (1) is not selected from The group consisting of [(2chlorophenyl)-benzimidazole-indolyl]methyl-pentanoic acid butyl decylamine and 2-(2-open-[u]-dioxane-baked 5_Base_Benzimidine small base) j benzyl-butanamine. Individually preferred are the compounds of formula (I) and each preferably is a physiologically acceptable salt thereof, and it is especially preferred that the compound of formula (10) is pharmaceutically acceptable H. The compound of formula (1) may have one or more asymmetric c atoms and may therefore exist as a mixture of 121967.doc-24-200811112, a mixture of diastereomers or an optically pure compound. Preferred compounds of formula (1) as described above are those compounds wherein ... is a C 1 -1 mercapto group, a low carbon alkoxy group - a low carbon alkyl group, a low carbon alkoxy group - a Wei group - a low carbon group , cycloalkyl, cycloalkyl-lower alkyl, phenyl, phenyl-lower alkyl, di-phenyl-lower alkyl, heterocyclic or heterocyclic-lower alkyl, wherein The cyclic group is selected from the group consisting of piperidinyl and 2-oxo-pyrrolidinyl, wherein the cycloalkyl, phenyl or heterocyclic group is optionally independently selected from the group consisting of 1 to 3 Substituents of the group are substituted with a lower alkyl group, a lower alkoxy group, a lower alkoxy group-carbonyl group, a morpholinyl group and a formamidine group. Preferably, R1 is alkyl, cycloalkyl or phenyl, wherein phenyl is optionally substituted with from 1 to 2 substituents independently selected from lower carbon alkyl. More preferably, R1 is 1,1,3,3-tetramethylbutyl, cyclopentyl, cyclohexyl or 2,5-dimethyl-phenyl. Other preferred compounds as defined above are those wherein R i is tetrahydronium, cycloalkyl substituted by 1 to 2 halogens or phenyl substituted by 1 to 2 lower alkyl groups, In particular, wherein Ri is tetrahydropyran-4-yl, 4,4-difluoro-loryl or 2,6-dimethyl-phenyl. Other preferred compounds of formula (1) as described above are those compounds wherein R2 is hydrogen. Further, preferred is a compound of the formula (1), wherein R3 is lower alkyl, cycloalkyl, partially unsaturated cycloalkyl, phenyl, phenyl-lower alkyl or heteroaryl, wherein the heteroaryl is selected from a group consisting of U-pyridyl and benzodioxenyl, wherein the phenyl or heteroaryl is optionally substituted with 1 to 3 substituents independently selected from the group consisting of: , lower alkyl, lower 121967.doc -25- 200811112 stone transalkoxy, NH2, N (H, lower alkyl) & N (lower alkyl) 2. Preferably, R is decyl, phenyl, phenyl-lower alkyl or pyridyl. More preferably, 11 is a cyclopentyl group, a cyclohexyl group, a phenyl group, a 3-phenyl-propyl group or an η-pyridine-2-yl group. Other preferred compounds are those wherein R3 is lower alkyl, tetrahydropyranyl or substituted with up to 3 substituents independently selected from fluoro-lower alkyl and fluoro-lower alkoxy Phenyl, preferably, wherein R3 is lower alkyl or tetrahydron-butyryl, more preferably wherein R3 is isobutyl, pentyl or tetraazaben-2-yl. Another preferred embodiment of the present invention relates to a compound of the formula (1) as described above, wherein R4 is a) a heteroaryl group selected from the group consisting of thienyl, pyrrolyl, h-side oxy-1 , 2-dihydro-pyridyl, fluorenyl, quinolyl and anthracene, 3 • di-oxy-isoindenyl, the heteroaryl group optionally being selected from low stone by i to 2 Substituted by a substituent of a group consisting of an alkyl group and a stupid group; b) a mesenyl group which is unsubstituted, or substituted, or a phenyl group which is substituted with three substituents independently selected from the group consisting of: Halogen, hydroxy, cyano-lower alkyl, lower alkoxy, lower alkyl-carbonyl, lower carbaryl-N(H), lower alkoxylate, amine continuation, Di-lower alkyl-amine sulfonyl, lower alkyl sulfonyl, thienyl, pyrazolyl, thiadiyl, succinyl, triterpene, tetradecyl, 2-tertoxy 2) each of the bite groups; or C) if R3 is a cycloalkyl group, R4 is a cycloalkyl group, and R4 may also be a phenyl group. Preferably, R4 is a) a heteroaryl group selected from the group consisting of: a base group, a 2' side oxy group -121967.doc -26 - 200811112 1 '2_one gas-0 ratio sigma group and quinoline a group wherein the thienyl group is optionally substituted with a phenyl group; or b) an unsubstituted naphthyl group or a phenyl group substituted with 1 to 2 substituents independently selected from the group consisting of: hydroxy-low carbon Alkyl, lower alkoxy, low sulphonyl-mono-n(h), sulphonyl or tetradecyl. Each of the options a), ... and c) given above constitutes a preferred embodiment individually. More preferably, R4 is 2,4-dimethoxy-phenyl, naphthalen-2-yl, 4-hydroxymethyl-phenyl, 4-(tetrazol-5-yl)-phenyl, 4-(imidazole) _2-kibphenyl, 4-ethlylamino-phenyl, 5-phenyl-thiophene-2-yl, 2-hydroxyl 4,2-dihydro-pyridyl-4-yl or hydrazine Other preferred compounds are those compounds, wherein R4 is a) a heteroaryl group selected from the group consisting of pyridyl, pyrazolyl, isoindole, benzo Strontium, fluorenyl, fluorenyl, σ, benzo[b]nonenyl, benzothiazolyl, benzofuranyl and quinoxalinyl, the heteroaryl is optionally Up to 2 substituents independently selected from the group consisting of halogen, CN, NH2, N (lower alkyl) 2, lower alkyl, lower alkoxy, fluoro-lower alkyl And morpholinyl; or b) unsubstituted naphthyl or naphthyl or phenyl substituted with 1 to 3 substituents independently selected from the group consisting of: an aminomethyl group, a pixel, a low carbon Alkyl, fluoro-lower alkyl, fluoro-lower alkoxy, lower alkenyl, N (lower alkyl) 2, N (H, lower alkyl) CO, benzene Acyl, phenoxy and optionally substituted with 1 to 3 substituents independently selected from fluoro _ ET and - lower alkyl substituents of the phenyl group. Further, preferably, R4 is a) a thienyl group substituted with #素; or b) a phenyl group substituted with an amine carbenyl group or a halogen. More preferably, 'R4 is 5·chloroindol-2-yl, 2-aminocarbonyl-phenyl or 4-chloro-phenyl. Each of the options a) and b) given above constitutes a preferred embodiment individually. Other preferred compounds of formula (1) as described above are those compounds wherein R, R, R7 and R8 are each independently H, halo, lower alkyl or lower alkoxy, or R6 and R7 are taken together A 6-membered aromatic carbocyclic ring is formed together with the carbon atom to which it is attached; especially such compounds, wherein rS, R6, y and R8 are each independently hydrazine, halogen or lower alkyl, or R6 & R7 are bonded together Together with the carbon atoms to which they are attached, a 6-membered aromatic carbocyclic ring is formed. ^佳地' R5 is hydrogen. Further, preferably, r6 is hydrogen, fluorine or methyl, more preferably hydrogen or methyl. Further, preferably, r7 is hydrogen, fluorine or chlorine, more preferably gas. Further, preferably, R8 is hydrogen. In particular, preferred compounds are the compounds of formula (I) and the pharmaceutically acceptable salts thereof, and the esters thereof, which are described in the examples as individual compounds. The compound of the formula (1) is a compound selected from the group consisting of 2,N-monohexyl, 2-(2phenyl-Zhidumei also 1 Ganbenzinzil (tetra)-1-ylethylidene Amine hydrochloride, 2-[2-(4·gas-phenyl)-benzoimidamine, 11 u]·4·methyl-pentanoic acid cyclohexyl ketone 121967.doc 28- 200811112 4-{1- [Cyclohexyl-(4-morpholin-4-yl-phenylaminecarbazyl)-methyl]-1H-benzimidazol-2-ylbenzoic acid methyl ester hydrochloride, 2,N-bicyclo Hexyl-2-[5,6-dichloro-2-(2,4-dimethoxy-phenyl)-benzimidazol-1-yl]-acetamide, 2-cyclohexyl-2-[2 -(2,4-dimethoxy-phenyl)-benzimidazol-1-yl]-N-isopropyl-acetamide hydrochloride, 2, Ν·dicyclohexyl-2-[2- (4-methoxy-phenyl)-benzimidazol-1-yl]-acetamide hydrochloride, 2,N-dicyclohexyl-2-[2-(3-methoxy-phenyl) -benzimidazol-1-yl]-acetamide hydrochloride, 2,N-dicyclohexyl-2-[2-(2-methoxy-phenyl)-benzimidazol-1-yl]- Acetamide hydrochloride, 2,N-di-f-hexyl-2-(2-na-1-yl-benzoquinone. Sodium-1-yl)-ethylamine hydrochloride, 2,N-di-bad Hexyl-2-[2-(3-ethyllacyl-phenyl)-benzoquinone -1 -yl]-ethanoamine hydrochloride, N-cyclohexyl-2-[2-(2,4-dimethoxy-phenyl)-benzimidazol-1-yl]-4-phenyl - Butanamine, N-cyclohexyl-2-[2-(2,4-dimethoxy-phenyl)-benzimidazol-1-yl]-3-methyl-butanamine hydrochloride, N-cyclohexyl-2-[2-(2,4-dimethoxy-phenyl)-benzimidazol-1-yl]-3-phenyl-propanamide hydrochloride, N-cyclohexyl- 2-[2-(2,4-Dimethoxy-phenyl)-benzimidazol-1-yl]-2-indolyl-2-yl-acetamide hydrochloride, 121967.doc -29 - 200811112 N-Cyclohexyl-2-cyclopentyl_2-[2_(2,4-dimethoxy-phenyl-benzimidazole β1_yl]-acetamide hydrochloride, 4-{1-[ Cyclohexyl-(cyclohexylaminecarbazinyl-methyl)]_1Η-benzimidazolylbenzoic acid methyl ester, 2, fluorene-dicyclohexyl-2-(2-naphthalen-2-yl-benzimidazolyl) ) _ acetamidine, 2,N-dicyclohexyl-2-[2-(3-thiophene-2-yl-phenyl)-benzimidazole-indole-yl acetamide, 2,N-bicyclo Hexyl-2-[2-(5-phenyl-thiophene-2-yl)> benzimidazolyl]-acetamide, 3-{1-[ ί chenyl-(cyclohexylaminecarboxamyl-methyl) Methyl benzimidazolylphthalate, 2-[2-(3·trans-phenyl-phenyl) -Benzene-salt small base] Heart methyl _ decanoic acid cyclohexyl ylamine, 21 (4, fluorenyl phenyl) benzoyl] _4_ fluorenyl pentanoic acid cyclohexyl decylamine, 醯 2 -[2-(1Η-吲哚-5-yl)-benzimidazole] Τ里·1"·yl]-4-methyl-pentanoic acid cyclohexylamine, brewing 2-[2-(m* 6-yl)-benzoxanthracene small group]_4_methyl-pentanoic acid cyclohexylamine, soil 2-[2-(4-amino-phenyll-benzimidazoleβ1_yl]_4_methyl _cyclohexylamine valeric acid, soil based]·Ν- 2-cyclohexyl-2-[2_(2,4-dimethoxy-phenyl)·benzoimidazole 4_((R)l-phenyl- Ethyl l-acetamide, base l·2,N-dicyclohexyl_2-[2-(4-hydroxymethyl-phenyl)-benzimidazole_ι_ 121967.doc •30- 200811112 , 裒hexyl 2-[2·(2,3-monomethoxy-phenyl)-benzoiminyl-indoleyl]_'phenyl-butanamine, 2-[2-(3-cyano) -phenyl)_benzimidazole_丨_yl]_2,N-dicyclohexyl-acetamide, 2,N-dicyclohexyl-2_{2-[4_(1h_tetrazole·5_yl)_ Phenylbenzimidazole <_ benzylamine hydrochloride, 3- [1-(benzylaminocarbamoyl-cyclopentyl.methyl)_1H_benzimidazole_2-yl] Methyl benzoate, 2-[2-(2,4-dioxin) Benzyl-phenyl)-benzimidazole _ 丨-yl]-hexanoic acid cyclohexyl decylamine, 2,N-dicyclohexyl-2-[2-(3-methanesulfonyl-phenyl)-benzimidazole _丨_ acetylamine hydrochloride, N-benzyl-2-cyclohexyl-2_[2_(2,4-dimethoxy-phenyl)-benzoxazole small group l·acetamide , 2_cyclohexyl-2-[2-(2,4-dimethoxy-phenyl)-benzopyranyl]A-servomethyl-butyl)-acetamide, 4_[1-( Methylbenzylaminomethyl-cyclopentyl-methyl>1H_benzimidazolyl]-benzoic acid methyl ester, 1 N-cyclononyl-2-[2_(3-methoxy-phenyl) _benzimidazole small decylamine hydrochloride, & 2,N-dicyclohexyl_2_[2_(2,4-dimethoxy-phenyl)_5-methyl-benzo-salt _ 1- Base]-acetamide hydrochloride, 2-[2-(4-chloro-phenyl)benzimid. Sitting on a small base]·2> Dicyclopentyldiamine amine 121967.doc -31- 200811112 acid salt, N-diphenylmethyl-2-cyclohexyl-2-[2-(2,4-dimethoxy -Phenylbenzimidazole_1-yl]-acetamide, N-benzyl-2-(2-naphthalen-1-yl-benzimidazole_ι_yl)-4_phenyl-butan Amine, 2-cyclohexyl-2-[2-(2,4-dimethoxy-phenyl)-benzimidazolyl]-indole-(4-methoxy-phenyl)-acetamide, 2, hydrazine -dicyclohexyl-2-[2-(2,4-dimethoxyphenyl)-4-indolylbenzimidazole-1-yl]-ethanoamine, 2, fluorene-dicyclohexyl-2 -{2-[3-(2-Sideoxy-Ethrolidineβ1_yl)·Phenyl]- benzophenidamine-1 -yl}-acetamide hydrochloride, 2, fluorene-dicyclohexyl _2-[2_(2-Sideoxy 4,2-dihydro-pyridinium-benzophenan-1 -yl]-acetamide, Ν-cyclopentyl-2-[2_(2-methoxy- Phenyl)-benzimidazole _i_yl]_4•phenyl-butanamine, 2-cyclohexyl-2_[2-(2,4-dimethoxy-phenyl)-benzimidazole] ]_n_pentyl·ethinamide, oxazol-1-yl]-2-cyclopentyl-acetamidine N-benzyl-2-[2-(4-chloro-phenyl)-benzoimide salt Acid salt,

2'N-«一土戍基- 2_(2 -Caiqi loan government I, not 1 base-benzimidazolyl)_acetamidine, 2-[2-(3-carbyl-phenyl)_ Benzene oxime on water-1·yl]·Ν-cyclohexyl-4-phenyl-butanamine, 2-[2·(4-hydroxy-phenyl)-benzimidazolyl]-4 amine hydrochloride , Ν-t-butyl 2-cyclohexyl-2methyl-pentanoic acid cyclohexyl hydrazine [2_(2,4-dimethoxy-phenyl)-benzopyrene sitting - 121967. Doc -32.  200811112 1 -yl]-acetamide, 4-[1-(1-benzylaminocarbamoyl-3-phenyl-propyl; oxime H-benzimidazol-2-yl]-benzoic acid Ester, 4-[1-(1-cyclohexylaminecarbazinyl-3-phenyl-propyl)-1Η-benzoimidazol-2-yl]-benzoic acid methyl ester, 2, fluorenyl-dicyclopentyl -2- [2-(2-methoxy-phenyl)-benzimidazole-1-yl]-acetamide, 2,N-dicyclohexyl-2-[2-(2,4-dimethyl Oxy-phenyl)-naphtho[2,3-d]imidazol-1-yl]-acetic acid amine 2-[2-(2,3·dimethyllacyl-phenyl)-benzo-salt- L-yl]-4 -mercapto-nonylcyclohexyl decylamine, N-benzyl-2-[2-(2-decyloxy-phenyl)-benzimidazol-1-yl]-4- Phenyl-butanamine, 2-cyclohexyl-2-[2-(2,4-dimethoxy-phenyl)-benzimidazol-1-yl]-N-(3-isopropyllacyl- Propyl)-ethanoamine '2-[2-(2,4-dimethoxy-phenyl)-benzimidazol-1-yl]-N-isopropyl-4-phenyl-butanamine , N·Benzyl·2-silverinyl-2-(2-na-1-yl-benzoquinone. Sodium-1 -yl)-Ethylamine, 2,N-dicyclohexyl-2-[ 2-(2,3-dimethoxy-phenyl)-benzimidazol-1-yl]-acetamide, 2-[2-(2,4-dimethoxy-phenyl)-benzo Taste. sit-1-yl]-4-methyl-decanoic acid ring Hexyl decylamine, 2-cyclohexyl-2-[2-(2,3-dimethoxy-phenyl)-benzimidazol-1-yl]-N-iso 121967. Doc -33· 200811112 propyl-acetamide, 2-[2-(2,3-dimethoxy-phenyl)-benzimidazole _丨_ kib N_isopropyl_4_phenyl- Butylamine, 2-[2-(4-acetamido-phenyl)-benzimidazolylpyridyl N-cyclohexyl-4-phenyl-butanamine, N-benzyl-2-[2- (4-Chloro-phenyl)-benzimidazolyl-4-phenyl-butanamine hydrochloride, 4-[1-(1-isopropylaminemethylmercapto-pentyl)-1Η_benzo Methyl imidazole_2-ylbenzoate, N-butyl-2-[2-(2,4-dimethoxy-phenyl)benzoimidazole-indenyl]_2_phenyl_acetamidine Amine, . -(^-(di-dimethoxy-phenyl-benzimidazole-indole-yl b'methyl-pentyl isopropyl decylamine, 2-benzopyrene, 3] dioxolane Dilute _5_yl_N_butyl_2_[2·(2,3-dimethoxy-phenyl)-benzimidazol-1-yl]•acetamidine, 2-benzo[1,3] M-trioxolane-5-yl | butyl 2_[2_(2,4-dimethoxy-phenyl)-benzimidazol-1-yl]-acetamide, Ν-butyl- 2-[2-(2,4-dimethoxyphenyl)benzimidazole-diyl]_2-(2-fluoro-phenyl)-acetamide, hydrazine-cyclopentyl-2-[2_ (3-hydroxy--laughing) V匕丞本基)_本开唑_丨_基]_4_phenyl-butanamine, 2-[2_(4_ethylindenyl)phenyl) 1·基]•Isopropyl hexanoate, butyl [2 (2,3·1 methoxy-phenyl)· 并 口 嗤 ] ] ] ] ] ] ] ] 12 12 12 12 12 12 12 12 12 12 12 12 12 12 12 Doc -34- 200811112 2-[2-(4-ethyl-benyl)_本其咪0圭-^基"μ"τ Lane-capric acid cyclohexyl decylamine, N-butyl-2·[2 -(2'3-dimethoxy. Phenyl)-benzopyrene small base] phenyl-acetamide, Ν-butyl-2-[2-(2,3-dimethoxy-phenyl)-benzimidazole small base Methoxy-phenyl)-ethinamide, Ν-butyl-2-[2_(2,3·dimethoxy-phenyl bup and ^ sit small base 仏 仏 · phenyl)-B Indoleamine, Ν-butyl-2-[2-(2,dimethoxy-phenyl)benzo-b-butyrazole small group]^(heart dimethylamino-phenyl)-acetamide, 2- [2-(2,3-Dimethoxy-phenyl)-benzopyranyl]-isopropyl isopropylamine, 4-{1-[(2-fluoro-phenyl)-isopropyl Aminyl-methyl]_lH-benzimidazolyl}-methyl benzoate, 2-[2-(3-cyano-phenyl)-benzopyrene-based cardamoyl-valeric acid ring Hexyl decylamine, 2-[2-(3-gas-phenyl)-benzopyrimidine-yl]_4_methyl-pentanoic acid cyclohexyl decylamine, N-butyl-2-[2_(2, 4-dimethoxy-phenyl)-benzoxazole small group]·2_(4-methoxy-phenyl)-ethylamine, N-benzyl-2-[2-(3-methoxy Benzyl-phenyl)-benzimidazole _ 丨-yl]_4_phenyl-butanamine hydrochloride, 2-(4- gas-phenyl)-2-[2_(2,3-dimethoxy) -phenyl)_benzimidazole_丨_yl]_N·isopropyl-acetamide, 121967. Doc -35- 200811112 and σm-sial-1-yl]-2-(4-di-N-butyl_2-[2-(2,4-dimethoxyphenyl)- benzylamino -phenyl)-acetamide, 2-[2-(4-carbyl-phenyl)benzoxanyl]isopropyl Iphenyl-butylamine, and imidazol-1-yl; μ'A _-valeric acid cyclohexyl hydrazine 2-[2-(4-hydroxy-phenyl)-aniline, 2-[2-(3- gas phenyl)-benzimamine, 1 yl] isopropyl- 4-phenyl-butyl N-butyl-2-(4- gas-phenyl)-2-[2»(2 1-yl)-ethonamide, 4-dimethoxy-phenylbenzene And imidazole _ 2-[2-(3·cyano-phenyl)·benzo-saltyl]-Ν-isopropyl_4_phenyl-butylamine, 2-ethyl-ethyl-phenyl)_ Benzoisoxazole·4]_ν_Isopropyl winter ("oxy-phenyl)acetamidine, MW isopropylaminecarbamyl-(4-methoxy-phenyl)-methyl]_m Methyl benzoxazol-2-ylbenzoate, 4-indole-(isopropylaminecarbamimido-phenylmethyl)-exidine-benzoxanthene-2-ylbenzoate , Ν-isopropylmethyl-1 Η "Big 2 _ _ _ _ benzopyranyl] ice phenyl-butanamine, 2-[2-(3-cyano-phenyl) benzene Iso-sodium sulfa-hexyl hexylamine, 2-[2-(4'-yl-phenyl)·benzo Methyl sulphate] _ pentyl valerate, 2-benzo[1,3]dioxolyl butyl-2_[2_(1_mercapto_ih_pyrrole-2 -yl)-benzimidazole·^-yl]-acetamide, 121967. Doc -36 - 200811112 2-Cyclohexyl-2-[2-(2,4-dimethoxy-phenyl)-benzoxamid-1-yl]indole (2,6-dimethyl-benzene) Ethylamine, 2, fluorene-dicyclohexyl-2-[2-(2,4-dioxalyl-phenyl)-benzopyrene, ethene, 2-cyclohexyl 3-alkenyl-indole-cyclohexyl-2-[2-(2,4-dimethoxy-phenyl> benzoimidazol-1-yl]-acetamide, 2-[2-(4 ·Cyano-phenyl)·benzophenazol-1-yl]-2, fluorene-dicyclohexyl·ethanoamine hydrochloride, 2-cyclohexylcyclopentyl·2-[2-(2,4 -dimethoxy-phenyl)-benzopyranyl]-acetamide, 2, fluorene-dicyclohexyl_2_[2_(2,4-dimethoxy-phenyl)_5,6-di Fluoro-benzoimylidene-1-yl]-acetamide, 2, fluorene-dicyclohexyl_2_[2_(2,4-dimethoxy-phenyl)_6-methyl-benzimidazole·1 -yl]-acetamide, 2-[2-(4-chloro-phenyl)-benzimidazole-; 1_ kib 2, Ν-dicyclohexyl-acetamide, 2, fluorene-dicyclohexyl _2_[2_(4_Aminesulfonyl-phenyl)·benzimidazole _ ι_ kibacetamide hydrochloride, 2-cyclohexyl-2-[2-(2,4-dimethoxy) _Stupyl)_Benzene-flavored salicyl-based ice (1,1,3,3-tetramethyl-butyl)-acetamide, 4-(1):cyclopentyl-( Amylamine methyl hydrazino-methyl]] ΐΗ 苯 benzophenidyl}-benzoic acid methyl ester hydrochloride, 2, Ν-dicyclohexyl-2_(2_quinoline salt, basic open imidazole-1 -yl)-acetamide hydrochloride 2-[2-(4-amino-phenyl)-benzimidazole small label J 2,JN-monohexyl-acetonitrile 121967. Doc -37- 200811112 Amine, 2J2-(2,4-di-f-phenyl)-benzimidazole-;[-yl]_5_phenyl-pentanoic acid cyclohexyl decylamine hydrochloride, 4-[ 1-(1-cyclopentylaminecarbazinyl-3-ylphenyl-propyl)_1H_benzimidazol-2-yl]-benzoic acid methyl ester, 2,N-dicyclohexyl-2-[2- (4-dimethylaminesulfonyl-phenyl)-benzimidazolyl]-acetamide hydrochloride, 2,N-dicyclohexyl-2·[2-(3-aminesulfonyl-benzene) Benzo-imidazolium- phenylethanide hydrochloride, 2, fluorene-dicyclohexyl-2-{2-[3_(1Η-tetrazol-5-yl)-phenyl]-benzoimidazole -Buji}-acetamide hydrochloride, 2,N-dicyclohexyl-2-{2-[4-(1Η-imidazol-2-yl)-phenyl]•benzimidazolyl}-acetamidine Amine hydrochloride, 2,N-dicyclohexyl-2-[2-(4-imidazol-1-yl-phenyl)-benzimidazole-^pyridylamine hydrochloride, 2,N-di Cyclohexyl-2·[2_(4-[1,2,4]triazol-4-yl-phenyl)-benzimidazole-diyl]-acetamide hydrochloride, 2, Ν·dicyclohexyl -2_{2_[4·(1Η_σBizozolyl)_phenyl]_benzimidazole-buki}-acetamide hydrochloride, 2, Ν-dicyclohexyl 丄 叩, 2,3] 嗔Azole_4_yl·stupyl)_benzimidazole·1-yl]-B Amine hydrochloride, 2, > 1_dicyclohexyl_2_[2_(1,3_di-oxy-2,3_dihydro·1Η_isoindolyl)-benzimidazole-1- ]]-acetamide hydrochloride, 2,N-dicyclohexyl_2_[2_(3_tetrazolyl)phenyl] benzoimidazole-1-yl]-B 121967. Doc -38- 200811112 Hydrazine hydrochloride 4-[ 1-(1⁄4-hexyl-3-methoxycarbonylphenylamine fluorenyl-methyl)_ih-benzimidazol-2-yl]- benzoic acid methyl ester Hydrochloride, hexyl-[(4-methoxycarbonyl-cyclohexylmethylamine fluorenyl]-methyl}-1 Ηbenzimidazole-2-yl)-benzoic acid methyl ester hydrochloride, 4 -{2-cyclohexyl_2-[2_(4-methoxycarbonyl-phenyl)-benzimidazole_ι_ kibethylaminopiperidine-carboxylic acid ethyl ester hydrochloride, Ν-ring Hexyl-2-anthracene (2,4-dimethoxyphenyl)benzoiminyldiyl-2-phenyl-acetamide hydrochloride, cyclic oxime oxime 対 対 ) ) Methylaminoglycolate methyl iodide-benzimidazol-2-yl)-benzoic acid methyl ester hydrochloride, 4_{1-[cyclohexyl-(3-methoxycarbonyl-propylaminecarbamyl)- Methyl]-1-benzoimidazole-2-ylbenzoic acid methyl ester hydrochloride, 4-{1-[cyclohexyl-(4-methoxycarbonyl-butylaminemethanyl)-methyl bromide Benzopyridin-2-yl}-benzoic acid oxime ester hydrochloride, 4-{1-[ 哀 己 - -(5-methoxycarbonyl-pentylaminemethyl hydrazide > methyl] _ old _Benzimidine-2-yl}-benzoic acid methyl ester hydrochloride, 2-cyclohexyl_2_[2-(2,4-dimethoxy . Phenyl)-benzopyrimidinyl]methyl-acetamide hydrochloride, small base] indolecyclohexyl-2-(2-(4-ethoxyphenylamino-phenyl)-phenyl Indoleamine, 2-[2-(3-ethoxyphenylamino-phenyl)-phenethylamine, and imidazol-1-yl]·2, fluorene-dicyclohexyl)methyl]- 1Η-stupid and 4-{1-[cyclohexyl-(3-carbamoyl-phenylamine-carbazide 121967. Doc -39- 200811112 Imidazol-2-ylbenzoic acid methyl ester hydrochloride, and N-% amyl-2-(2-naphthalen-1-yl-benzoquinone 17 m °-1-yl)-prop Amine, and its pharmaceutically acceptable salts and esters. Particularly preferred compounds of the formula (I) are those compounds selected from the group consisting of N-cyclohexyl-2-[2-(2,4-dimethoxy-phenyl)-benzimidazole 丨·2·pyridin-2-yl-acetamide hydrochloride, N-cyclohexyl-2·cyclopentyl_2_[2_(2,4-dimethoxy-phenyl)-benzoxazole _ 乙基]_acetamide hydrochloride, 2, Ν-- ί ^ hexyl-2-(2-naphthalen-2-yl-benzimidazol-1-yl) acetamidine, 2, N-di Cyclohexyl 2_[2_(5-phenyl·thiophene-2-yl)-benzimidazolyl]•acetamidine, 2,N-dicyclohexyl_2-[2-(4-hydroxymethyl-benzene) Benzomidazolyl]-acetamide, 2,N-dicyclohexyl-2-{2_[4_(1h tetrazol-5-yl)-phenyl]•benzimidazole small group}-acetic acid amine Hydrochloride, 2,N-dicyclohexyl_2_[2_(2,4. Dimethoxy-phenyl)_5•methyl-stupid salivary-1-1-yl]-acetamide hydrochloride, 2,N-dicyclohexyl-2-[2_(2-olyloxy), 2_Dinitrogen "Bit + base" _ benzo-b-azol-1-yl]-acetamide, ', 2_cyclohexyl-2-[2-(2,4-dimethoxy-phenyl) _Benzimidazole small group] also (2,6-diamidino-phenyl)-ethylamine, 2-cyclohexyl-N-cyclopentyl o-(2,4.dimethoxy-phenyl) _benzimidazole _ bromo]-acetamide, 121967. Doc 40- 200811112 2-Cyclohexyl-2-[2-(2,4-di-foxy-phenyl)-benzopyrimidin-yl]-Ν_ (1,1,3,3-tetramethyl -butyl)-acetamide, 2,N-di-hexyl-2-(2-quinolin-6-yl-benzimidazole-; 1-yl)-acetamide hydrochloride, 2-[2 -(2,4-methoxy-phenyl)-benzimidazole _ 丨-yl]phenyl-pentanoic acid cyclohexyl decylamine hydrochloride, 2,N-dicyclohexyl-2-{2-[4 -(1Η-imidazol-2-yl)phenyl]benzimidazole small group}-Ethylamine hydrochloride, N-cyclohexyl-2-[2-(2,4-dimethoxyphenyl) Benzo-saltyl-p-phenyl-acetamide hydrochloride, and 2-[2-(4-acetamido-phenyl)-benzimidazole-fluorenyl-]-] Hexyl acetamamine, and pharmaceutically acceptable salts and esters thereof. Other preferred compounds of formula (I) are those compounds selected from the group consisting of 2,N-dicyclohexyl_2_(2 _Phenyl-benzimidazole 丨 丨 基 基 ,, 2_[1-(cyclohexyl-cyclohexylamine fluorenyl-fluorenyl)_1H_benzimidazole _2 benzyl benzoate, [based -.Bis-2-yl)-benzo.m. sit a small base]-2,N-dicyclohexyl-acetamide, 2,N-dicyclohexyl-2-[2·(2-ethyl _5 _Methyl-2H-pyrazol-3-yl)-benzopyrimidine|Sit-1_yl]-acetamide, '-cyclohexyl-2-[2·(5-methyl-isophenanth-4 -Base)·Benzimindole_1_yl]_Ethylamine, 121967. Doc 200811112 2,N-Dicyclohexyl-2-[2-( 1H-pyrrol-2-yl)-benzimidazole-1·yl]acetamide, 2-(1Ή-[2,5']biphenyl And imidazol-1-yl)-2, fluorene-dicyclohexyl-acetamide, 2, fluorenyl-di- hexyl-2-(2-n-butyl-2-yl-benzoquinone 17 m -1--1-yl )-Ethylamine '2-[6->Smelly-2-(4-chloro-phenyl)-benzoquinone-salt-yl]_2, Ν-dicyclohexyl-ethonamide, 2-[ 6-Gas-2-(4-chloro-phenyl)-benzimidazol-1-yl]-2, fluorene-dicyclohexyl-acetamide, 2-[2·(4-chloro-phenyl)- 6-methoxy-benzoquinone-flavored σ-l-yl]-2, fluorene-dicyclohexyl-acetamide, 2-[6-chloro-2-(4-chloro-phenyl)-5-fluoro -benzoquinone miso-1-yl]-2, fluorene-dicyclohexyl·acetamide, (S)-2,N-dicyclohexyl-2·[2-(2,4-dimethoxy- Phenyl)-benzimidazol-1-yl]-acetamide, (S)-2-[2-(4- gas-phenyl)-benzoquinone-l-yl]-2, fluorene-di Cyclohexyl-ethylamine, 2-[1-(cyclohexyl-cyclohexylaminecarbazinyl-indenyl)-1Η-benzoimidazol-2-yl]-indole-methyl·benzamide, 2, Ν-Dicyclohexyl-2-(2-furan-3-yl-benzimidazol-1-yl)-acetamide, 2,N-dicyclohexyl-2-indole (3-methyl-furan-2 -base)-benzo Imidazolium-1·yl]-acetamide, 2,N-dicyclohexyl-2-[2-(3-methyl-isoxazole-5-yl)-benzimidazol-1-yl]-acetamidine Amine, 2,N-dicyclohexyl-2(2-m-tolyl-benzimidazol-1-yl)-acetamide, 121967. Doc-42- 200811112 2,N-Dicyclohexyl-2-[2-(3-fluoro-phenyl)-benzimidazol-1-yl]-acetamide, 2,N-dicyclohexyl-2- [2·(2-Phosphate·Phenyl)-benzoquinone-flavored σ-l-yl]-ethylamine ' 2,Ν-dicyclohexyl-2-[2·(3,5-dimethyl-iso) Oxazol-4-yl)benzimidazol-1-yl]-acetamidamine, 2, fluorene-diclofen-2-[2-(3-methyl-11secen-2-yl)-phenylhydrazine taste. -1--1-yl]-acetamide, 2, fluorene-dicyclohexyl-2-[2-(4-vinyl-phenyl)-benzimidazol-1-yl]-acetamide, 2, hydrazine -dicyclohexyl-2-[2-(2,3-dimercapto-phenyl)-benzimidazol-1-yl]-acetamide, 2, fluorene-dicyclohexyl-2-[2_(3 , 4-didecyl-phenyl)-benzimidazol-1-yl]•acetamidine, 2, fluorene-dicyclohexyl-2-[2-(4-ethyl-phenyl)-benzimidazole -1-yl]-acetamide, 2, fluorene-dicyclohexyl 2 -[2-(2,4-dimethyl-phenyl)-benzimidazol-1-yl]-acetamide, 2 , Ν-dicyclohexyl-2-[2-(2-ethyl-phenyl)-benzimidazol-1-yl]•acetamidine, 2, fluorene-dicyclohexyl-2-[2-(4 -fluoro-3-methyl-phenyl)-benzimidazol-1-yl]-acetamide, 2, fluorene-dicyclohexyl-2-[2-(3-fluoro-4-methyl-phenyl )-benzimidazol-1-yl]-acetamide, 2, fluorene-dicyclohexyl 2 -[2-(2,6-difluoro-phenyl)-benzimidazol-1-yl]-B Guanamine, 121967. Doc -43- 200811112 2,N-Dicyclohexyl-2-[2-(3,5-difluoro-phenyl)-benzimidazol-1-yl]-acetamide, 2,N-disepine - 2-[2·(2,5-di-phenyl)-phenylhydrazine 117 m嗤-1-yl]-ethinamide, 2, fluorene-dicyclohexyl-2-[2-(3,4 -difluoro-phenyl)-benzimidazol-1-yl]-acetamide, 2, fluorene-di-d-hexyl-2- [2-(2,3-di-phenyl)-phenylhydrazine 17 m °坐-1-yl]•Ethylamine, 2,Ν-dicyclohexyl-2_[2-(1Η-indol-4-yl)-benzimidazol-1-yl]-acetamide, 2, Ν_二断己基-2-[2-(1Η-ϋ引ϋ朵-6-yl)-benzoquinone ϋ ϋ-1 -yl]-ethylamine, 2-[2-(5-gas- σ 吩 -2 - - - - -2 - 嗤 嗤 ] ] ] Ν Ν Ν Ν 二 二 二 二 二 2- 2- 2- 2- 2- 2- 2- 2- 2- 2- 2- 2- 2- 2- 2- 2- 2- 2- 2- 2- 2- 2- 2- 2- 2- 2- 2- 2- 2- 2- 2- 2- 2- 2- 2- 2- 2- 2- 2- 2- 2- 2- 2- 2- 2- 2- -1-yl]-2, fluorene-dicyclohexyl-acetamide, 2-[2-(2-ethylindenyl-phenyl)-benzimidazol-1-yl]-2, fluorene-dicyclohexyl - acetamidine, 2, fluorene-bis-hexyl- 2- [2-(4-isopropyl-phenyl)-benzoquinone-1 -yl]-ethanoamine, 2-[2-(4 -Cyano-2-fluoro-phenyl)-benzimidazol-1-yl]-2, fluorene-dicyclohexyl-acetic acid amine, 2, fluorene-dicyclohexyl-2-[2-(2-dimethyl Amino-phenyl )-benzimidazol-1-yl]-acetamide, 121967. Doc-44- 200811112 2,N-Dicyclohexyl-2-[2-(3-dimethylamino-phenyl)-benzimidazol-1-yl]-acetamide, 2,N-bicyclo Hexyl-2-[2-(4-decyloxy-3-methyl-phenyl)-benzimidazol-1-yl]-ethanoamine 2,N-dicyclohexyl-2-[2-( 4. Methoxy-2-methyl-phenyl)-benzimidazole-1_yl]-acetamide, 2, fluorene-dicyclohexyl-2-[2-(3-oxilyoxy-4-oxime 2-phenyl)-benzimidazol-1-yl]-acetamide, 2, fluorene-dicyclohexyl-2-[2-(2-ethoxy-phenyl)-benzimidazol-1-yl ]-acetamide, 2-[2-(6-gas-° than 唆-3-yl)-benzoquinone ρm嗤-1 -yl]·2, Ν-di-d-hexane-ethylamine, 2- [2-(2 - gas-0 to 唆-4 · yl)-benzoquinone 1 ^ m σ sit-1-yl]-2, Ν -di-d-hexane-ethylamine, 2-[2-(4- Gas-phenyl)-6-gas-benzoquinone. Sit _1_yl]-2, Ν-di-dihexyl-ethylamine, 2,N-dicyclohexyl-2-[2-(3-fluoro-4-indolyl-phenyl)-benzimidazole -1-yl]·acetic acid amine, 2-[2-(4- gas-3-methyl-phenyl)-benzoquinone-propen-1-yl]_2,N-dicyclohexyl-acetamide, 2 -[2-(3- gas-2-methyl-phenyl)-benzoquinone-1 -yl]-2,N-dicyclohexyl-acetic acid amine, 2-[2-(4- gas-3 - gas-phenyl)-phenylhydrazine °-1-yl]-2,N-dicyclohexyl-ethylamine, 121967. Doc -45- 200811112 2-[2-(3 -Gas-4·Gas-Phenyl)-benzoquinone-l-yl]-2,N-dicyclohexyl-ethanoamine, 2,N-di Cyclohexyl-2-[2-(5-methyl-1H-indol-2-yl)-benzimidazol-1-yl]-acetamide, 2,N-dicyclohexyl-2-[2- (2,3,4-Trifluoro-phenyl)-benzimidazol-1-yl]-acetamide, 2,N-dicyclohexyl-2_[2-(2,4,5·trifluoro-benzene -benzimidazol-1-yl]-acetamide, 2-(2-benzo[b]thiophen-2-yl-benzimidazol-1-yl)-2, fluorene-dicyclohexyl-B Indoleamine, 2, fluorene-dicyclohexyl-2·[2-(5-fluoro-1Η_吲哚-2_yl)-benzimidazolyl-1-yl]-acetamide, 2 - (2-benzene弁°塞σ sits -6-yl-benzoquinone ρ 吐-1 -yl)-2, Ν-dicyclohexyl-ethinamine, 2, fluorene-dicyclohexyl-2-[2-(4-iso Propoxy-phenyl)-benzimidazol-1-yl]-acetamide, 2, fluorene-dicyclohexyl-2-[2-(3,4-dimethoxy-phenyl)-benzo Imidazol-1-yl]-acetamide, 2, fluorene-dicyclohexyl-2-[2-(2,5-dimethoxy-phenyl)-benzimidazol-1-yl]-acetamide , 2, Ν-dicyclohexyl-2-[2-(2-difluoromethoxy-phenyl)-benzimidazol-1-yl]-acetamide, 2, fluorene-dicyclohexyl-2 [2-(4_difluoromethoxy) - phenyl) - benzoimidazol-l-yl] - as acetamide, 121,967. Doc -46- 200811112 2,N-Dicyclohexyl-2-[2-(3-difluoromethoxy-phenyl)-benzimidazoleacetamide, 2,N-dicyclohexyl-2-[2 ·(4_Trifluoromethyl_phenyl)_benzimidazole_丨_yl]-acetamide, 2,Ν-dicyclohexyl-2-[2-(3,4-dichloro-phenyl) _benzimidazole-fluorenyl-ylacetamide, 2-[2-(4-Molyl)-benzimidazole + keb (10) dicyclohexyl-acetamide, 2, fluorene-dicyclohexyl- 2-[2-(6-methoxy-naphthalene-2-yl)-benzimidazole 丨 丨 基 基 ,, 2,N-dicyclohexyl-2-[2-(3-trifluoromethyl) Oxy-phenyl)-benzimidazole 丨 基 基 ] ] ] 2 2 2 2 2 2 2 2 2 2 2 2 2 2 2 2 2 Imidazolyl]-acetamide, 2,N-dicyclohexyl-2·[2-(3-fluoro-4-trifluoromethyl-phenyl)benzimidazole-yl-ylamine-acetamide, 2 ,>^Dicyclohexyl-2_[2-(6-diethylamino)pyridin-3-yl)-stanoimidazolyl-1yl]-ethanoamine '2-[2_(2·气_5 _Methyl-phenyl)-benzoxazole small group]_2, fluorene-bicyclohexylamine, 2-[2-(5-chloro-2-methyl-phenyl)_ stupid 17 m Salivation small base]_2,]^-bicyclohexylamine, 2-[2_(2_chlorobutyl-phenyl)_ stupid Small oxazol-yl] ^ qe dicyclohexylamine Yi Amides, 2, Ν- _2- dicyclohexyl (2-quinol-6-yl - imidazol-1-yl and Ben > as acetamide, 121,967. Doc -47- 200811112 2-[2-(5-Chloro-2-fluoro-phenyl)-benzimidazol-1-yl]·2, fluorene-dicyclohexyl-acetamide, 2, fluorene-bicyclic Hexyl 2-[2-(4-methoxy-3,5·dimethyl-phenyl)-benzimidazole-1-yl]-acetamide, 2, fluorene-dicyclohexyl-2-[ 2-(2,3-dimethoxy-phenyl)-benzimidazol-1-yl]-acetamide, 2-[2-(3-chloro-4-hydrazino-phenyl)-benzene弁1:7 m-sial-1-yl]-2, fluorene-dicyclohexyl-acetamide, 2, fluorene-dicyclohexyl-2-[2_(2,5-dichloro-phenyl)-benzo Imidazolyl-1-yl]-acetamide, 2-[2-(3-chloro-2,4-dioxa-phenyl)-benzo. Micun-1-yl]-2,^^ Dicyclohexyl·Ethylamine, 2-[2-(2-chloro-4,5-difluoro-phenyl)-benzimidazol-1-yl]- 2, Ν-dicyclohexyl-acetamide, 2, fluorene-dicyclohexyl-2-[2-(4-diethylamino-phenyl)-benzimidazol-1-yl]·acetamide , 2-[2-(4-Benzyldecyl-phenyl)-benzimidazol-1-yl]-2, fluorenyl-dicyclohexyl-acetamide, (S)-2-[2-(4 - gas-phenyl)-benzoquinone-l-yl]-2, fluorene-dicyclohexyl-ethenylamine, 2, fluorene-dicyclohexyl-2-[2-(4-phenoxy- Phenyl)-benzimidazol-1-yl]-acetamide, 2, fluorene-dicyclohexyl-2-[2.(2-phenoxy-phenyl)-benzimidazol-1-yl]- Acetamine, 121967. Doc -48- 200811112 2,N-Dicyclohexyl-2-[2-(3-phenoxy-phenyl)-benzimidazol-1-yl]-acetamide, 2,N-dicyclohexyl_ 2-{2-[2-(1,1,2,2-tetrafluoro-ethoxy)-phenyl]-benzimidazol-1-ylethylamine, 2,N-dicyclohexyl-2 -{2-[3-(1,1,2,2-tetrafluoro-ethoxy)-phenyl]-benzimidazole-1-yl}-acetamide, 2,N-dicyclohexyl-2 -{2-[4_(1,1,2,2-tetrafluoro-ethoxy)-phenyl]-benzimidazole-l-yl}-acetamide, 2,N-dicyclohexyl-2- [2-(4'-trifluoromethyl-biphenyl-4-yl)-benzimidazol-1-yl]ethylamine, 2,N-dicyclohexyl-2-[2-(3f,4^ Dichloro-biphenyl-4-yl)-benzimidazol-1-yl]-acetamide, 2,N-disuccinyl- 2- [2-(2,4-di--5-amine acid) Base-phenyl)-benzoquinone 11-sodium-1 -yl]-ethonamine '(S)_2-[6-gas-2-(4·gas-phenyl)-5-gas-benzoquinone.圭-1_基]-2, Ν·二J 己己基-acetamide, 2, Ν - ί 哀 己 -2 -2 - (2 ° ° than σ -2 - 2 - phenyl-benzoquinone 11 m σ sit - 1 · 基)-Ethylamine ' 2; ^- diazepine-2-[2-(6-methyl-yl)-benzo. Mic-l-yl]-acetamide, 2,N-dicyclohexyl-2-[2-(3-methyl-pyridin-2-yl)-benzimidazol-1-yl]-acetic acid amine, 2,N·二 哀 己 - - 2- [2-(6-Methyl-0 to 17-den-2-yl)-benzoindole 吐-1 · yl]-acetamide, 2-[2- (2-Amino-pyridin-3-yl)-benzimidazol-1-yl]-2, fluorenyl-dicyclohexyl-ethyl 121967. Doc -49- 200811112 Indoleamine, 2-[2-(6-cyano-acridin-3-yl)-benzimidazol-1-yl]-2,N-dicyclohexyl-acetamide, 2, N-dicyclohexyl-2-[2·(2-methoxyindole-1-yl)-benzimidazole-1-yl]-acetamide, 2-[2-(2- gas-6 - fluorenyl σ ratio -3-yl)-benzo- succinyl-1 -yl]-2,N-di-di-hexyl-acetamide, 2-[2-(2- gas-6-methyl- °比ϋ-4-yl)-benzo-salt-s-l-yl]-2, fluorene-dioxahexyl-acetamide, 2, fluorene-di-dextyl-2 - (2 - 啥琳-3 -yl-benzoquinone ϋ · · 1 -yl)-ethinamine ' 2, Ν -di-dihexyl-2 - (2 - 啥 · 4 - yl-benzoquinone saliva-1 -yl)-B Amine amine '2-[2-(3•gas-4-trifluoromethyl-phenyl)-benzimidazol-1-yl]-2, indole-dicyclohexyl-acetamide, (S)-2 -[2-(4- gas-phenyl)-benzoquinone 17 m 唆-1-yl]-4-methyl-pentanoic acid decyl decylamine, 2-(4-chloro-phenyl)-2-[ 2-(4-Chloro-phenyl)-benzimidazol-1-yl]-N-cyclohexyl-acetamide, 2-[2-(4- gas-phenyl)-benzophenanthrenequinone-1_ ]-Ν-ϊ辰己基-2-(4-dimethyl fluorenyl-phenyl)-acetamide, 2-[2-(4-chloro-phenyl)-benzo-α--1-yl ]-Ν-ϊ辰己基- 2- (3,4- Dichloro-phenyl)-acetamide, 2-[2-(4-chloro-phenyl)benzoquinone 1^m. -1--1-yl]-N-dextyl-2-(3-methoxy-phenyl)-acetamide, 2-[2-(4- gas-phenyl)-benzoquinone 0 sitting-1 -yl]-N-low hexyl-2-p-tolyl-ethyl 121967. Doc -50- 200811112 Amine, 2-[2-(4- gas-phenyl)·benzoquinone-flavored σ-l-yl]-N-cyclohexyl- 2-(3- gas-phenyl)_ B Amine, 2-[2-(4-gas-phenyl)-benzoquinone-l-yl]-N-lymphoterolyl-2-(4-dimethoxymethoxyphenyl)-acetamide , 2-[2-(4-Chloro-phenyl)-benzimidazol-1-yl]-N-cyclohexyl-2-(2,5-difluoro-phenyl)-acetamide, 2-[ 2-(4- gas-phenyl)-benzoquinone-flavored σ-l-yl]hexyl-2-(2-oxo-5-methoxy-phenyl)-acetamide, (S)-2- [2-(5-Gas-2-Gas-Phenyl)-benzoquinone 11 m σ sitting-1-yl]-2, Ν-二 哀 己 _ _ _ _, (8)-2,^^- Di-m-hexyl-2-[2-(2,3-dimethoxy-phenyl)-benzoquinone 11-spin-1-yl]-acetamide, (S)-2-[2-(3 - Gas-4-methyllacyl-phenyl)-benzoquinone m-sodium-1-yl]-2, Ν-di 哀 己 基-acetamide, (S)-2-dextyl- 2- [2 -(2,4-dioxaoxy-phenyl)-benzopyridinium-l-yl]-indole_(2,6-dimethyl-phenyl)-acetamide, 2-[2- (4-gas-phenyl)-benzoquinone 1:7 m squat-1 -yl]-2- 哀 己 基-Ν-(4,4-di-cyclohexyl)-acetamide, (S) -2-[2-(4-Ga-phenyl)-benzoquinone m. Sodium-1 -yl]-2-dextyl-indole-(4,4-dioxa-3⁄4-hexyl)-ethonamine '(S)-2-[2-(2-amino-indole-3- Base) - benzoquinone. Rice bran sits -1 -yl]-2,N-dicyclohexyl-acetamide, 2,N-lymphoterol-2-(6-gas-2-0-bit bite-2-yl-benzoquinone -1 - base) - B brewed 121967. Doc -51 - 200811112 Amine, 2,N-dicyclohexyl-2-[2-(2,4-dimethoxy-phenyl)-6-fluoro-benzimidazol-1-yl]-acetamide , 2,N-Dicyclohexyl-2-[6-fluoro-2-(4-methoxy-phenyl)-benzimidazol-1-yl]-acetamide, 2,N-dicyclohexyl- 2-[2-(2,3-difluorophenyl)-6-fluoro-benzimidazol-1-yl]-acetamide, 2,N-dicyclohexyl-2-[2_(2,3- Dimethoxy-phenyl)-6-fluoro-benzimidazol-1-yl]-acetamide, 2,N-dicyclohexyl-2-[2-(2-ethyl-5-methyl- 211-pyrazol-3-yl)-6-fluoro-benzimidazol-1-yl]-acetamide, 2,N-dicyclohexyl-2-[2-(3,5-dimethyl-iso Oxazol-4-yl)-6-fluoro-benzimidazol-1-yl]-acetamide, 2,N-dicyclohexyl-2-[6-fluoro-2·(1Η-pyrazole-4- -benzimidazol-1-yl]-acetamide, 2, fluorene-dicyclohexyl-2-[2-(1,5-dimercapto-1Η-pyrazol-3-yl)·6- Fluoro-benzimidazol-1-yl]-acetamide, 2, fluorene-dicyclohexyl-2-[6-fluoro-2-(3-methyl-isoxazol-5-yl)-benzimidazole -1-yl]-acetamide, 2, Ν·dicyclohexyl_2-[6-fluoro-2-(lH-upyrrol-2-yl)-benzimidazol-1-yl]-acetamidine Amine, 2,N-di-f-hexyl-2-[6-gas-2-(3-methyl-[sigma] -2 -yl)-benzo-1:7 m σ sit-1·yl]-acetamide, Ν-benzyl-2-[2-(4-chloro-phenyl)-benzimidazole-1- Base]-2-cyclohexyl-acetamidine 121967. Doc -52- 200811112 Amine, N-butyl-2-[2-(4- gas-phenyl)-benzoquinone-l-yl]-2-cyclohexyl-ethonamide, 2-[2_( 4-oxo-phenyl)-benzimidazol-1-yl]-N-cyclohexyl-2-(tetrahydro-piperidin-4-yl)-ethonamide 2-[5-chloro-2-( 4-chloro-phenyl)-6-fluoro-benzoquinone 1:7 m indol-1-yl]-2,N-dicyclohexyl_acetamide, 2-[2-(4- gas-phenyl) -5,6-difluoro-benzoquinone °°-1-yl]-2, Ν·dicyclohexyl _ acetamidine, 2-[2-(4-chloro-phenyl)-benzoquinone 1-yl]-2-cyclohexyl-indole-(tetrazine-pyran-4-yl)-acetamide, 2-[2·(4- gas-phenyl)-benzoquinone. -1--1-yl]-2-cyclohexyl-fluorene-cyclopropyl-ethylamine, 2, fluorene-dioxahexyl-2-[2-(6-nor--4-yl-° ratio σ -3-yl)-benzoquinone 0-sodium-1_yl]-acetamide, (S)-2-[2-(4- gas-phenyl)-benzoquinone °-1-1-yl]-2 -cyclohexyl-fluorene-(tetrazo-bran-4-yl)-ethonamine '(S)-2,N-dicyclohexyl-2-[2·(4·methanesulfonyl-phenyl) -benzimidazol-1-yl]-acetamide, (S)-2-[2-(4- gas-phenyl)-benzoquinone 11 mil-1-yl]-2 - cumyl-indole Cyclopropyl-acetamide, 2-[6-chloro-2-(4-chloro-phenyl)-5-fluoro-benzimidazol-1-yl]-N-cyclohexyl-2-(tetrahydro-喃 -4--4-yl)-acetamide, (S)-2-[2-(4- gas-phenyl)-benzoquinone-1 -yl]-N-nupentyl-2-(tetrazine - Brigade 121967. Doc •53- 200811112 4-(4-)-ethylamine, (S)-2-[6-chloro-2-(4-chloro-phenyl)-5-fluoro-benzimidazol-1-yl] -N-cyclohexyl-2-(tetrazine-pyr-4)-ethylamine, (S)-2-[2-(4-chloro-phenyl)-5,6-difluoro-benzene And imidazol-1-yl]-2,N-dicyclohexyl-ethylamine, (S)-2-[2-(5-gas-dexoster-2-yl)-benzoquinone 1:1 m σ -1--1-yl]_2,N-dicyclohexyl·acetamide, (S)-2,N-dicyclohexyl-2-[2-(2,3-difluoro-phenyl)·6-fluoro -benzimidazol-1-yl]-acetamide, 2-[6-chloro-2-(4-chloro-phenyl)-5-fluoro-benzimidazol-1-yl]-indole-cyclohexyl- 2-cyclopentyl-acetamide, (S)-2-[6-chloro-2-(4-chloro-phenyl)-5-gas-benzopyran-l-yl]-heptanoic acid cyclohexyl Indoleamine, (S)-2-[6-gas-2-(4- gas-phenyl)-5-gas-benzoquinone-l-yl-N-lycopene- 2-cyclopentyl -acetamide, 2-[2·(4- gas-phenyl)-5-gas-benzoquinone-l-yl]-2,N-dicyclohexyl-ethylamine, 2-[1- (cyclohexyl-cyclohexylamine-methylindenyl-methyl)-5,6-difluoro-1H-benzoimidazol-2-yl]-benzoic acid methyl ester, 2,N-diylhexyl-2 - ( 5,6 - 二气-2 - ° than bite-2 - base - benzophene m 0 sit -1 - base) - B Indoleamine, 2-[2-(5-aero-σ-sept-2-yl)-5,6-diox-benzoquinone-flavored β-l-yl]-2, fluorene-dicyclohexyl-acetamidine Amine, 2-[6-gas-1-(5 哀 基  坏 基 胺 - - - - 甲基 甲基 甲基 甲基 甲基 12 12 12 12 12 1967 1967 1967 1967 1967 1967 1967 121967. Doc -54- 200811112 Methyl oxazol-2-yl]-benzoate, 2-(6-gas-5-gas-2-° ratio σ-denyl-2-benzoquinone m ^-1 -yl)- 2,N-di-homohexyl·acetamide, 2-(6-gas-5-gas-2-σ ratio sigma-3-yl-benzoquinone 17 m sal-1-yl)-2, fluorene-di Bad hexyl-acetamide, 2-(6-gas-5- cis-4-yl-benzophenanthene-1-yl)-2, fluorene-dicyclohexyl acetamide, 2-[6 - gas - 2-(3 - gas - σ-phenant-2-yl)-5 - gas - benzoquinone ° guan-1-yl]-2, Ν-dicyclohexyl-acetamide, 2-[6 ·Gas- 2-(5-Gas-σ-cephen-2-yl)-5-Gas-Benzo- σ-m σ-l-yl]-2, fluorene-dicyclohexyl-acetamide, (S) -2-[6-gas-2-(4- gas-phenyl)-5-disorganized-benzophenanyl-sodium-1-yl]-3-ethyl-decanoic acid cyclohexylamine, 2-[6 - Gas-5-chaotic - 2-(4- gas-phenyl)-benzoquinone. -1--1-yl]-2,N-dicyclohexyl_acetamidamine, 2-[2-(4- gas-phenyl)-benzoquinone-flavored 17-spin-1-yl]-2-s-hexyl-N -( 1 -isopropyl-2-methyl-propyl)-acetamide, 2-[6_gas- 2-(4- gas-phenyl)-5· gas-benzoquinone 1:1 mΰ -1 -yl]-2 - hexyl-N-cyclopentyl-acetamide, 2-[2-(4-chloro-phenyl)·5,6-difluoro-benzimidazol-1-yl ]-Ν-cyclohexyl-2·(tetrahydroendan-4-yl)-ethonamide, (S)-2-[2-(4-a-phenyl)-5-fluoro-benzimidazole- 1-yl]-2, fluorene-dicyclohexyl-acetamide, 2-[2-(4-phenylphenyl)-5,6-diox-benzopyrene 0-l-yl]-2- Cyclohexyl-Ν- (four 121967. Doc -55- 200811112 Nitrogen-Burethane-4 -yl)-acetic acid amine, 2-[6-chloro-2-(4-chloro-phenyl)-5-fluoro-benzimidazol-1-yl]-2 -cyclohexyl-N-(tetrahydro-l-tetra-n-yl)-acetic acid amine, 2,N-dicyclohexyl-2-[2-(3-dimethylamino-phenyl)-5,6 -difluoro-benzimidazol-1-yl]-acetamide, 2,N-dicyclohexyl-2-[2-(3-didecylamino-phenyl)-6-fluoro-benzimidazole -1-yl]-acetamide, 2-[2-(4- gas-phenyl)-5,6-disorder·benzoquinone σ sit-1-yl]-2-dextyl-N· (1 _ isopropyl-2 -methyl-propyl)-ethonamide '2-[6-gas-2-(4- gas-phenyl)-5-a-benzo-indol-1-yl ]-2-cyclohexyl-indole_(1-isopropyl-2-methyl-propyl)-ethonamide '2-[2-(3- gas-phenyl)-5,6-di-benzene-benzene弁17米峻-1-yl]-2, Ν-dicyclohexyl _ acetamidine, 2-[2-(2- gas-phenyl)-5,6-diox-benzo-jun-l- ]], Ν-dicyclohexyl _ acetamidine, (S)-2-[6-gas-5-fluoro-2-(4-fluoro-phenyl)-benzimidazol-1-yl]- 2, Ν_dicyclohexyl-acetamide, (S)-2-[2-(4-chloro-phenyl)-5,6-digas-benzo π-spin-1·yl]-Ν- Cyclohexyl-2-(tetrahydro-cun-4-yl)-ethonamide, 2-[2-(4- gas-phenyl -5 - gas - phenylhydrazine 11 m σ sit-1-yl]-oxime-cyclohexyl-2-(tetrazine · brim-4)-ethylamine, 2-[2-(4-chloro- Phenyl)-6-gas-benzo-salt-l-yl]-indole-cyclohexyl-2-(tetrachloro-indolyl-4-yl)-ethonamide, 2·[2-(4- Chloro-phenyl)-6-fluoro-benzoimidazol-1-yl]-indole-cyclohexyl-2-(tetrahydro- 121967. Doc -56- 200811112 σ辰喃-2 -yl)-acetic acid amine 2-[6-Gas-2-(4·Ga-phenyl)-5-Gas-Benzene-flavor- sitting--1-yl]- N-cyclohexyl-2·(tetrahydro-piperidin-2-yl)-acetamide, (S)-2?N---------[6- -11-cephen-2-yl)-benzo σm° _ 1 -yl]-acetic acid amine '(S)-2-[2-(2- gas-phenyl)-5,6-difluoro- Benzoquinone 11 m 嗤-1-yl]-2, fluorene-dicyclohexyl-acetamide, (S)-2-[2-(4- gas-phenyl)-5-gas-benzophene methane -1-yl]-indole-cyclohexyl-2-(tetrazine-bungan-4-yl)-ethonamide, (S)-2-[2-(4- gas-phenyl)-6-gas -Benzene-flavor 11-spin-1 -yl]-N-suppleyl-2 (tetrahydro-0-n-butyl-4-yl)-ethanoamine, (S)-2-[2-(4-chloro-benzene (6)Fluoro-benzimidazol-1-yl]-N-cyclohexyl-2-(R)-tetrazine-l-butan-2-yl-ethylamine, (S) -2-[2-( 4- gas-phenyl)-6-gas-benzoquinone °-1-yl]-N-cyclohexyl-2-(S)_tetrahydro-piperidin-2-yl-acetamide, 2- [2-(4- gas-phenyl)-5-gas-benzoquinone σ-l-yl]·N-lymphoterol-2-(tetrazine·bran-2-yl)-ethonamide ' 2, Ν-dicyclohexyl-2-[2-(3,4-di-phenyl)_6-methoxy-benzimidazol-1-yl]-ethyl '2-[2-(4- gas-phenyl)-6-methoxy-benzoquinone-flavored 0-l-yl]-2, fluorenyl-dicyclohexyl-acetamide, 2-[2-( 5·Gas-σ-cephen-2-yl)-6-methoxy-benzoquinone ρ米σ sitting-1-yl]-2,Ν-dicyclohexyl-acetamide, 2-[2_(3- Gas-4-methoxy-phenyl)-6-methoxy-benzoimidazole-1-yl]-2, Ν- 121967. Doc -57- 200811112 Dicyclohexyl-acetamide, 2-[2-(4- gas-3-fluoro-phenyl)-6-decyloxy-benzo-salt-l-yl]-2,N -dicyclohexyl-acetamide, 2-cyclohexyl-N-cyclopentyl-2-[2-(3,4-dichloro-phenyl)-6-methoxy-benzimidazol-1-yl ]-acetamide, N-cyclohexyl-2-cyclopentyl-2-[2-(3,4-dichloro-phenyl)-6-nonyloxy-benzimidazol-1-yl]-B Indoleamine, 2-[2-(4-carbo-yl)-6-methoxy-benzoquinone-salt-1 -yl]-2-d-hexyl-N-cyclopentyl-acetamide, 2- [2-(3- gas-phenyl)-6-methyllacyl-benzoxamis-1-yl]-2,N-dicyclohexyl-acetic acid amine, 2,N-di-s-decyl- 2 - [2-(3,4-Di-phenyl-phenyl)-6-methoxy-benzoquinone-flavored σ-l-yl]-acetamide, 2-[2-(4- gas-phenyl)- 6-Methyl-benzophenone-flavored α-l-yl-yl]-indole-yttrium-based 2-cyclopentyl-acetamide, 2-[2-(4- gas-3-phenyl-phenyl) -6-Methyl- benzoyl-benzoquinone-n-yl]-2 - 哀 己 基 _ 环-cyclopentyl-acetamide, 2-[2·(3- gas-4-methoxy- Phenyl)-6-methoxy-benzo-benzo-1-yl]-2-cyclohexyl-indole- ί 戍 - - 乙 乙 ^ ^ 2 2 Ν 2 二 二 二 二4-fluoro-phenyl)-6-methoxy-benzimidazole-1 -yl]-acetamide, 2-[2-(3- gas-phenyl)-6-methoxy-benzo-s-s--1-yl]-2-cyclohexyl-N-cyclopentyl- Acetamide, 2-[2-(3-chloro-4-methoxy-phenyl)-6-methoxy-benzimidazol-1-yl]·Ν-ring 121967. Doc -58- 200811112 Hexyl-2-cyclopentyl-acetamide, 2-[2-(5-gas-sodium-2-yl)-6-methoxy-benzopyranyl-2-cyclo Amyl-acetamide, keb N-cyclohexylmethoxy-benzom 2·cyclobutyl-N-cyclohexyl-2-[2_(3,4-dichloro-phenyl)-6-azole-1 -yl]-acetamide, cyclohexyl _ 1 yl] bicyclo 2_[2-(5-a-indol-2-yl)-6-methoxy-benzo π m sal _ N-cyclopentyl -Ethylamine, 2-[2-(6-chloro-tolyl-3-yl)-6-methoxy-benzimidazolylhexyl-acetamide, 2-[2-(3-chloro-benzene) Base)-6-methoxy-benzophenanthrene. Sit_ι_ 戊基-乙含胺, 卞]卞·cyclohexyl: cyclo 2-[2-(3- gas-4-methoxy-phenyl)_6_decyloxy_stupidyl]-2 ΚΓ Dicyclopentyl-acetamide, 2, fluorene-dicyclohexyl-2-[6-methoxy-2-(6-trifluoromethyl-pyridine·3·美)~,, imidazole·1- 2-[2-(5-Gas-thiophen-2-yl)-6-methoxy-benzopyrene 4, Wangbuji]-2-cyclobutyl_N- Cyclohexyl-acetamide, 2-[2_(3_chloro-phenyl)·6-methoxy-benzomethylene]_2-cyclobutyl-cyclohexyl-acetamide, and Ν-cyclohexyl I Cyclopentyl·2_[2_(4·fluoro-phenyl)-6-methoxy·benzosin-1-yl]-acetamide, and pharmaceutically acceptable salts and esters thereof. Other particularly preferred compounds of formula (1) are those selected from the group consisting of the following: 121967. Doc -59- 200811112 2-[1-(cyclohexyl·cyclohexylaminecarbazyl-methyl)-1-benzoimidazole-2-yl]-benzoguanamine, (S)-2,N- Dicyclohexyl-2-[2-(2,4-dimethoxy-phenyl)-benzimidazol-1-yl]-acetamide, (S)-2-[2-(4-chloro- Phenyl)·benzimidazol-1-yl]-2,N-dicyclohexyl-acetamide, (S)-2-[2-(4-chloro-phenyl)-benzimidazol-1-yl ]-4-methyl-pentanoic acid cyclohexylamine, 2·[2-(4-Gas-phenyl)-benzoquinone.坐-1-基]-7V- 哀 己 基 - 2- (4-dioxamethyl phenyl)-acetamide, (S)-2-cyclohexyl-2-[2-(2,4- Dimethoxy-phenyl)-benzimidazol-1-yl]-#-(2,6-dimethyl-phenyl)-ethonamide '(S)-2-[2-(4- gas -Phenyl)-benzoate. -1 -yl]-2-oxahexyl-7V-(4,4-difluoro-cyclohexyl)-acetamide, (S)-2-[6-Ga-2-(4-N-phenyl-phenyl) )-5 - chaotic-benzoquinone-flavor-1-yl]-7V-cyclohexyl 2-(tetrazine-n-nan-4-yl)-ethonamide, (S)-2-[2-(5- Gas-σ phenant-2-yl)-benzo σm σ sit-1 -yl]-2,7V-di-fake hexylamine, (S)-2-[6-gas-2-(4 -Chloro-phenyl)-5-fluoro-benzoimidazol-1-yl]-heptanoic acid cyclohexyl decylamine, 2-[6-gas-2-(4- gas-phenyl)-5-gas-benzene Astringent 11-l-yl]-2-cyclohexyl-7V_(tetrahydropyran-4-yl)-acetamide, 2-[2-(3-nitro-phenyl)-5,6-difluoro -Benzene miso-1.yl]-2, #-dicyclohexyl-acetamide, 121967. Doc -60- 200811112 (S)-2,N--^-hexyl_2_[6_fluoro_2彳3_methyl_thiophene-2-yl)_benzimidazole-1-yl]•acetamidine, (S) 2 [2-(2-Gas-phenyl)_5,6-difluoro-benzimidazole_丨·yl]_2,N-dicyclohexyl-acetamide, (S)-2-[2 -(4•chloro-phenyl)·6_fluoro-benzimidazole_丨_yl]_n_cyclohexyl_2_(8)-tetrahydro-bran-2-yl-acetamide, (S)-2- [2-(4'Chloro-phenyl)·b-benzophenanthrene m]_N cyclohexyl winter (8)_tetrahydro-pyran-2-yl-acetamide, and 2-[2-(4-gas- Phenylfluoro-benzimidazole-1-yl]-indole-cyclohexyl-2-(tetrahydro-pyran-2-yl)-acetamide, and pharmaceutically acceptable salts and esters thereof. The compound of the formula (I) in the present invention may be derivatized at a functional group to provide a derivative which is converted into a parent compound in vivo. The present invention further relates to a method for producing a compound of the formula (1) as defined above. The method comprises cyclizing a compound of formula (II) to r1\

Wherein Ri, R2, R3, ^R, R, R6, R7 and R8 are as defined above. Ring of compound of formula (II)

It is carried out under the reaction conditions well known to those skilled in the art. Such a simple, s A x , band may be present, for example, in a suitable 121967.doc • 61· 200811112 > gluten in a gluten at a suitable temperature in a suitable reagent such as free pph or resin. Go on. The invention also relates to a compound of formula (1) as defined above, which is prepared by a process as described above. Compounds of formula (1) can be prepared by methods known in the art or as described below. Unless otherwise indicated, the substituents R1, r2, R3, r4, r5, r6, r7 and R8 are as defined above. The compounds of formula (I) of the present invention can be prepared, for example, by the methods and procedures given below. A typical procedure for the preparation of compounds of formula I is illustrated in the scheme below.

In a suitable organic solvent such as MeOH, the so-called type reaction (step a 'typical procedure can be found, for example, in Gr〇ss and Meienhofer"

Peptides, Volume 2,

In Academic Press, N.Y., 1980, pp. 365-381, 2-azidoarylamine j, carboxylic acid 2, isonitrile 3 and aldehyde 4 are condensed to 5. In the subsequent intramolecular (4) singular-type reaction with a suitable reagent such as PPh, the azidobisguanamine 5 can be converted to benzimidazole, which can optionally be carried out by using a strong base such as NaH or LiHMDA. Protonation and subsequent treatment with an alkylating agent R2-X (wherein X is a typical leaving group such as C1, Br, I, s〇2 alkyl, s〇2 fluoroalkyl, S〇2 aryl) N-alkylation (step c). Many basic components 2-4, especially carboxylic acid 2, are commercially available. If it is not commercially available, it can be 121967.doc -62- 200811112

Commercially available starting materials are prepared using procedures described in the literature and procedures generally known to those skilled in the art. Isonitrile 3 can be obtained, for example, by dehydrating the corresponding formamidine N (10) with a suitable reagent such as carbon brewing gas, POCls or Me2N=CH+cl cr, for example from a corresponding alcohol by using, for example, a high nail acid Preparation of a suitable oxidizing agent of propylammonium (VII). 2_azidoarylamine! Usually prepared from the corresponding 2-aminoaryl carboxylic acid in three steps, the stalk is diazotized by NaN 〇 2 = suitable solvent (for example methanol) and then a suitable azide salt such as ν_ Treatment is carried out to convert to 2_azidoarylcarboxylic acid. Subsequently, activation is carried out by 2-azidoarylcarboxylic acid by using a suitable reagent such as cholesteryl ethyl acetate (in the presence of a base such as triethylamine) and then a suitable azidation The anion source (sodium azide) is treated to obtain a nitrile aryl formate nitride-like rearrangement, which converts the resulting azidoaryl carboxylic acid into hydrazine. 2_Azidoarylamine i or 2 which can be obtained by activating a quinone-based carbamic acid with a suitable reagent such as ethyl benzoate in the presence of a base such as triethylamine and then treating with ammonia Preparation of _ azido aryl carbamide. The indoleamine is converted to i in a so-called Chinese rearrangement by treatment with a suitable reagent such as Na〇Br2. If the starting material or one of the compounds of formula (1) contains one or more functional groups which are unstable or reactive under the reaction conditions of one or more of the reaction steps, prior to the application of the key steps of the method known to the art. Introduce appropriate nucleus bases (eg, for example, at tw·Greene and PGM Wutts, Protective

Groups in 〇rgame chemistry", 2nd edition, 1991, Wiley NY). These protecting groups can be removed in the post-synthesis stage using standard methods described in the literature. 121967.doc • 63 - 200811112 When the compound (1), (2), (3) or (4) contains a stereosymmetric center, the compound (1) can be obtained as a mixture of diastereomers or enantiomers, which can be, for example, (for palmity). Isolation by HPLC or crystallization is well known in the art. Racemic compounds can be separated, for example, by crystallization from optically pure acid or by specific chromatography using an antagonist or palmitic eliminator. Separation of its enantiomers via diastereomeric salts.Another method of preparing a compound of formula I is illustrated in the following scheme.

k RM6 carbon fluorenyl group in the process, again in the type condensation, a single b 〇 c_ protected o-aryl aryl diamine 6, carboxylic acid 2, isonitrile 3 and aldehyde 4 in an organic solvent such as methanol in acid Condensation to bis-indoleamine 7 in the presence of (such as HCl) (step a). The bisguanamine is deprotected with TFA and cyclized to the desired benzimidazole [(step b), which may optionally be deprotonated with a strong base (eg NaH or LiHMDA) and subsequently with an alkylating agent R2-X (wherein X is a typical leaving group such as c, Br, j, s〇2 alkyl, s〇2 gas alkyl, S〇2 aryl) and N-alkylated (step uniform) can be applied to A typical procedure for the method (for example) is described by et al. in Ding Let. 2001, 仏 4959_4962 and 4963_4968 or by z/ et al. in Tet. Lett 2004, 6757-6760. Single boc-protected neighboring The diamine 1 is commercially available or can be used from the corresponding unprotected diamine by the use of two 121967.doc-64-200811112 dicarbonate in the presence of a base such as diisopropylethylamine in an organic solvent such as THF. Prepared by treatment with a third butyl ester. Functional groups (such as _c〇2 alkyl, amine, cyano, and others) present in the 'I can be used as is typical of the standard procedures known to those skilled in the art (eg, LlA1H4 reduces the -C〇2 alkyl group to -ch2oh, the -co2 alkyl group is hydrolyzed to C〇2H and then converted to the indoleamine as appropriate, and the amine is thiolated) a functional group. If one of the starting materials or a compound of formula (I) contains one or more functional groups which are unstable or reactive under the reaction conditions of one or more reaction steps, it is well known in the art. Appropriate protecting groups can be introduced before the key steps of the method (eg, for example, in Tw·Greene and PGM· Wutts, Protective)

Groups in Organic Chemistry", 2nd edition, 1991, as described in Wiley Ν·Υ·). These protecting groups can be removed in the later stages of synthesis using standard methods described in the literature. If compound (3), Where (3), (4) or (6) contains a stereosymmetric center, the compound (1) can be obtained as a mixture of diastereomers or enantiomers, which can be, for example, by HPLC or crystallization. Separation by methods well known in the art. Racemic compounds can be passed through diastereomers, for example, by crystallization with optically pure acid or by specific chromatography using an off-parent for the palm adsorbent or the palmate dissolving agent. The salt is separated into its enantiomers. The steps in the above-described schemes &amp; and b or step a, the R present in (1) can be converted to other R or via other R1 using one reaction step or a series of reaction steps. Displacement. Two possible examples are given below: a) Rl = CH2Ph can be removed, for example, using de-benzylation conditions (for example, in a solvent such as methanol in a catalyst such as Pd(0)/carbon powder Under hydrogen 121967.doc -65- 200811112 solution) For example) by deprotonating the resulting CONHR2 with a strong base such as LiHMDA and using an alkylating agent such as C1 'Br, I, 8〇2 alkyl, S〇2 fluoroalkyl, A typical leaving group of the S 〇 2 aryl group, and Ri is 0 〇 1 〇 alkyl, lower alkoxy lower alkyl, lower alkoxy-carbonyl _ lower alkyl, cycloalkyl, naphthenic Treatment with a base-lower alkyl group, an aryl-lower alkyl group, a di-aryl-lower alkyl group, a heteroaryl-lower alkyl group or a heterocyclic group-lower alkyl group or by Pd(II) Promote the coupling of Ri-XCR1 to an aryl or heteroaryl group and X to C1, Br, or [or OSO2CF3] to introduce a new R1. b) (I)-CRSCONR^R2- Part of the decylamine is decomposed into 〇Κ3 (: hydrazine can be carried out using suitable conditions such as heating in isopropanol in the presence of NaOH or LiOH. The amine amide bond can then be formed using the amine HNWr2 and a typical peptide coupling agent such as EDCI, DCC or TPTU. Functional groups that are unstable or reactive under the reaction conditions of one or more of the reaction steps present in the protective group (I) may be protected by a suitable protecting group (eg, for example, at TW Greene and PGM) prior to the critical steps of the methods well known in the art. · Wutts &quot;Protective Groups in Organic Chemistry,, 2nd ed., 1991, Wiley Ν·Υ_). These protecting groups can be removed in the post-synthesis stage using standard methods described in the literature. Conversion of a compound of formula (I) to a pharmaceutically acceptable salt can be carried out by treating the compound with a mineral acid such as a hydrohalic acid (such as hydrochloric acid or hydrobromic acid) or other inorganic acid. (such as sulfuric acid, nitric acid, dish acid, etc.) 'The organic acid such as acetic acid, sulphuric acid, maleic acid, succinic acid, tartaric acid, methane sulfonic acid or p-toluene sulfonic acid. Salts formed with inorganic or organic acids can be obtained by standard methods known to those skilled in the art, for example 121967.doc • 66- 200811112 by dissolving a compound of formula (1) in a suitable solvent such as dioxane or THF, plus appropriate The corresponding acid of s is obtained. The product can conveniently be separated by filtration or chromatography. If a carboxyl group is present, the corresponding carboxylated salt can be prepared from a compound of formula (1) by treatment with a physiologically compatible base. A possible method of forming the salt is, for example, by adding 1/n equivalent of an alkaline salt such as M(〇H)n (wherein metal or phosphonium cation and n = hydroxide ion number) The solvent is removed from the solution in a suitable solvent (eg, ethanol, ethanol-water mixture, tetrahydrofuran-water mixture &amp;) and evaporated or lyophilized. Conversion of a compound of formula (1) to a pharmaceutically acceptable ester can be carried out, for example, by using, for example, benzotriazol-1-yloxy ginseng (dimethylamino) hexafluorophosphate scale (BOP), N, N- Dicyclohexylcarbodiimide (DCC), N_(3-dimethylaminopropyl)-Ν'-ethylcarbodiimide hydrochloride (EDCI) 4〇_(丨,2-二a condensing agent having a hydrogen 1 side oxy group which is smaller than pyridine group)-N, n, n, n_0 _ methyl fluorene tetrafluoroboric acid (TPTU) is treated with a carboxylic acid such as acetic acid to treat a hydroxyl group present in the molecule to produce a carboxy group. Ester or carboxy guanamine. Further, the carboxyl group present in the compound of the formula (1) can be reacted with a suitable alcohol under the similar conditions as described above. Where the preparation of the compound of formula (I) and all intermediates is not described in the examples, it can be prepared according to a similar method or as set forth above. The starting materials are either commercially available or known in the art. As described above, the novel compounds of the present invention have been found to bind to fxr and selectively activate FXR. It can therefore be used to treat and prevent diseases modulated by the agent. These diseases include increased levels of lipids and cholesterol, especially high LDL-cholesterol, high triglycerides, low HDL-cholesterol, lipid abnormalities, atherosclerosis, diabetes, especially non-insulin dependent sugars 121967.doc -67- 200811112 Urinary diseases, metabolic syndrome, cholesterol gallstones, cholestasis/liver fibrosis, cholesterol absorption diseases, cancer, especially gastrointestinal cancer, osteoporosis, peripheral obstructive diseases, ischemic stroke, Parkinson's disease (4) , s diSeaSe) and / or Alzheimer's disease (Alzheimer, disease). - Accordingly, the present invention is also directed to a pharmaceutical composition comprising a compound as defined above and a pharmaceutically acceptable carrier and/or adjuvant. The present invention also encompasses a compound as described above for use as a pharmaceutically active substance', particularly as a therapeutic remedy for the treatment and/or prevention of diseases mediated by FXR agonists, especially for the treatment and/or prevention of Disease medicine, live food, shellfish, lipid and cholesterol content, high cholesterol, high glycerol-酉曰, low HDL-cholesterol, lipid abnormalities, atherosclerosis diabetes, non-insulin-dependent diabetes, metabolic syndrome, cholesterol bile Stones, bile accumulation / liver fibrosis, cholesterol absorption disease, cancer, colon cancer, osteoporosis, peripheral obstructive disease, ischemic stroke, Parkinson's disease and / or Alzheimer's disease. In another embodiment of the present invention, the present invention relates to a method for treating and/or preventing a disease modulated by an FXR agonist, in particular for treating and/or preventing the following diseases: a decrease in lipid and cholesterol content, and a high ldl _Cholesterol, high glycerin, low HDL-cholesterol, lipid abnormalities, atherosclerosis, diabetes, non-Tengol-dependent diabetes, metabolic syndrome, gallbladder g] alcohol, gallstones, cholestasis/liver fibrosis, Montcanol absorption of disease, cancer, colon cancer, osteoporosis, peripheral obstructive disease, ischemic stroke, Parkinson's disease and/or Alzheimer's disease, the method involves administering to humans or animals A compound as defined. 121967.doc -68- 200811112 The invention also encompasses the use of a compound as defined above for the treatment and/or prophylaxis of diseases modulated by FXR agonists, especially for the treatment and/or prophylaxis: lipids and cholesterol Increased content, high LDL-cholesterol n-glycerol, low HDL_cholesterol, lipid abnormalities, atherosclerosis, diabetes, non-insulin-dependent diabetes, metabolic syndrome, biliary (four) gallstones, bile accumulation / Liver fibrosis, cholesterol-absorbing disease, cancer, gastrointestinal cancer, osteoporosis, peripheral obstructive disease, ischemic typhoid, Parkinson's disease, and/or Alzheimer's disease. The invention also relates to the use of a compound as described above for the preparation of a medicament for the treatment and/or prophylaxis of a disease modulated by an FXR agonist, in particular for the preparation of a medicament for the treatment and/or prophylaxis of the following diseases Uses: increased lipid and cholesterol levels, high LDL_cholesterol, high glycerol triglyceride, low HDL-cholesterol, lipid abnormalities, atherosclerosis, diabetes, non-insulin dependent diabetes, metabolic syndrome, cholesterol gallstones, bile Siltation/liver fibrosis, cholesterol absorption disease, cancer, gastrointestinal cancer, osteoporosis, peripheral obstructive disease, ischemic stroke, Parkinson's disease and/or Alzheimer's disease. The agents comprise a compound as described above. Preferably, it is for preventing and/or treating high LDL-cholesterol content, high triglyceride, lipid abnormality, cholesterol gallstone, cancer, non-Tengol-dependent diabetes and metabolic syndrome, and particularly preferably high orphan cholesterol. High triglyceride content and lipid abnormalities. a The following test was carried out to determine the activity of the compound of formula (1). The background information of the combined verification can be found in Nichols JS et al., &quot;~~. (iv) For example, 〇f 121967.doc -69- 200811112 scintillation proximity assay for peroxisome proliferator-activated receptor gamma ligand binding domain’', (1998) Anal. Biochem. 257: 1 12-1 19. Construction of bacterial and mammalian expression vectors to produce glutathione-s-transferase (GST) and Gal4 DNA binding domain (GAL) protein fused to the human FXR (aa 193-473) ligand binding domain (LBD) . To achieve this, the sequence portion encoding the FXR LBD was PCR amplified from the full length pure line by polymerase chain reaction (PCR) and subsequently colonized in the plastid vector. The final pure line was confirmed by DNA sequence analysis. Induction, expression and subsequent purification of the GST-LBD fusion protein were carried out in E. coli (five co//) strain BL21 (pLysS) cells by standard methods (Current Protocols in Molecular Biology, edited by Wiley Press, Ausubel et al). . Radioligand Binding Assay The binding of the test substance to the FXR ligand binding domain is assessed in a radioligand displacement assay. The assay was carried out in a buffer consisting of 50 mM Hepes (pH 7.4), 10 mM NaCl, 5 mM MgCl2. For each well in a 96-well plate, 40 nM GST-FXR LBD fusion protein was combined with 10 pg of glutathione citrate SPA beads (Pharmacia Amersham) in a final volume of 50 μΐ by shaking. Adding a radioligand (eg 40 ηΜ) 2, Ν-dicyclohexyl-2-[2-(2,4-dimethoxy-phenyl)-benzimidazol-1-yl]-acetamide, The reaction was incubated for 30 minutes at room temperature in the presence of the test compound followed by scintillation proximity counting. All 121967.doc -70-200811112 binding assays were performed in 96-well plates and the amount of bound ligand was measured using OptiPlates (Packard) on a Packard TopCount. Dose response curves were performed over a concentration range of 6χ10·9 Μ to 2·5χ10_5 。. Luciferase Transcription Reporting Gene Assay Baby hamster kidney cells (ΒΗΚ21 ATCC CCL10) were grown in DMEM medium containing 10% FBS at 37 ° C in an atmosphere of 95% 02: 5% CO 2 . Cells were seeded at a density of 105 cells/well in 6-well plates and subsequently transfected with pFA-FXR-LBD or expression plastids. Transfection lines were achieved using Fugene 6 reagent (Roche Molecular Biochemicals) according to the proposed protocol. Six hours after transfection, cells were harvested by trypsinization and seeded in 96-well plates at a density of 104 cells/well. After the cells were allowed to adhere for 24 hours, the medium was removed and replaced with 1 〇〇 μΐ of the phenol red-free medium (final DMSO concentration: 0.1%) containing the test substance or the control ligand. After the cells were incubated with the substance for 24 hours, 50 μM of the supernatant was discarded and then 5 μ μ of luciferase luminescence reagent (Roche Molecular Bio chemicals) was added to lyse the cells and start the luciferase reaction. Luminescence as a measure of luciferase activity was detected in a Packard TopCount. The transcriptional activation in the presence of the test substance is expressed as a fold change in luminescence compared to the luminescence of the cells cultured in the absence of the substance. The EC" value is calculated using the XL fitting program (ID Business Solutions Ltd. UK). The compound of the formula (1) has preferably from 0.55 nM to 1 〇μΜ in at least one of the above assays (EC50 or IC50), more preferably 〇 • Activity from 5 nM to 100 nM. For example, the following compounds show the following EC5〇 and IC5Q values in the binding assay described above: 121967.doc -71 - 200811112 By example ec50 ic5〇[μΜ] [μΜ] 2 0.7 1.5 34 Λ υ·086 0.5 A pharmaceutical preparation in the form of a fine, parenteral or topical administration. The pot may be administered by such means as oral, for example, in the form of lozenges, coated lozenges, dragees, hard gelatin. Capsules and soft gelatin capsules, solutions in the form of emulsions or suspensions; in the form of a rectum, for example in the form of a suppository; parenterally, for example in the form of an injection solution or suspension or infusion solution; or topical, for example as an ointment' cream or oil The form of the preparation is preferably administered orally. The preparation of the pharmaceutical preparation can be carried out by a method which is familiar to those skilled in the art by using the compound of the formula 1 and/or its pharmaceutically acceptable salt. View I* month status and other The combination of therapeutically useful substances is accomplished by the formation of a galenical administration form, together with a suitable non-toxic, inert or medicated solid or liquid carrier material and, if desired, a conventional pharmaceutical preparation. Suitable carrier materials are not only inorganic carrier materials but also organic carrier materials. Thus, for example, lactose, corn starch or derivatives thereof, talc, stearic acid or salts thereof can be used as lozenges and coated lozenges. Carrier materials for sugar-coated pills and hard gelatin capsules. Suitable carrier materials for soft gelatin capsules are, for example, vegetable oils, waxes, fats and semi-solid and liquid polyols (however, depending on the nature of the active ingredient, In the case of soft gelatin capsules, the carrier may not be required. Suitable carrier materials for the manufacture of solutions and syrups are, for example, water, polyols, sucrose, inert sugars and the like. Suitable carriers for injectable solutions 121967 .doc -72- 200811112 Agent substances are, for example, water, alcohol, _ a ^ ^ 矸 兀 、, glycerol and vegetable oils. Suitable carrier materials for suppositories are d + liquid or liquid Enzymes. ^. Suitable carrier materials for topical preparations are glycerides, semi-synthetic glycerol safflower, gans and 3 glycerides, hydrogenated oils, liquid waxes, liquid paraffins, liquid fatty alcohols, earth # a ^ Knowing, polyethylene glycol and cellulose derivatives. Consider # stabilizer, decadent, W, moisturizer and emulsifier, consistency improvement: no improvement, salt used to change osmotic pressure, buffer substance , solubilizing W, coloring, and masking agents and antioxidants as pharmaceutical adjuvants. The dosage of the compound of formula I can be determined according to the disease, the age of the patient and the individual condition; (: 堇4 # /, , And the wide range of sputum changes and, of course, in individual cases, should meet individual needs. For adult patients, consider a daily dose of about g to 1000 mg, especially about 1 gua to 300 mg. Depending on the severity of the disease and the precise pharmacokinetic profile, the compound can be administered in one or several daily dosage units, for example 1 to 3 dosage units. The pharmaceutical preparation conveniently contains W 500 mg, preferably (10) tons of phantom compound 0. [Embodiment] The following examples are intended to illustrate the invention in more detail. However, it is not intended to limit the scope of the invention in any way. Example abbreviations: Ηα=hydrochloric acid, HPLC=high pressure liquid chromatography, NaHc cadaveric sodium bicarbonate, Na2S04=^L sodium, pS_carbonate=from commercial 9〇〇_〇h (Acros Cat. 3〇134 5〇〇〇) Polystyrene prepared from a saturated CaC〇3 aqueous solution 121967.doc -73- 200811112 Ether-supported carbonate, PS-TsNHNH2=Polystyrene-loaded benzenesulfonyl hydrazine (Aldrich 532320-5g) , Si02 = silicone. General Notes When appropriate, the reaction is carried out under a nitrogen or argon atmosphere. Example 1 2,N-Dicyclohexyl-2-(2-phenyl-benzimidazol-1-yl)-acetamide hydrochloride 1.1 Addition of benzoic acid (34.2 mg, 0.28 mmol, 1 ·1 equivalent) Toluene-burned formic acid (42.6 11^, 0.3 8 111111〇1, 1.5 equivalents), isocyanatocyclohexane (30.6 mg, 0·28 mmol, 1.1 equivalents) and N-tert-butoxycarbonylphenyldiamine (52.1 mg, 0.25 mmol, 1 eq.) in MeOH (5 mL). A 1 M HCl solution (1 mL) was added and the mixture was taken from a gas (2X1 mL). Na2SO4 (50 mg), PS-carbonate (4 mmol/g, 50 mg) &amp;PS-TsNHNH2 (4 mmol/g, 50 mg) was added to the organic phase and the mixture was shaken for 60 minutes. The mixture was filtered and the filtrate was evaporated in vacuo. Purification by preparative HPLC (gradient elution: water with 〇························································ ) -Amino]phenylbutylaminodecanoic acid tert-butyl ester, 64 mg (47%). MS (ES + ) ·· 534 (M+H) 〇1.2 Add Concentrated HC1 (25% in water, 0.5 mL) to {2-[benzylidene-4-cyclohexyl-cyclohexylaminecarboxamyl-methyl a solution of -amino]phenyl}-aminocarbamic acid tert-butyl ester (64 mg, 0.12 mmol) in methanol (2.0 mL). The mixture should be heated under stirring in a focused microwave (CEM DiScovery) at Ι4ς&gt; M C for 3 minutes with stirring. The reaction mixture was then evaporated to give a solution of 2,N-dicyclohexyl-2-(2-phenyl-benzophenoneamine hydrochloride, 46 mg (850 / 〇). ES+) : 416 (M+H) 〇 Example 2 2-[2-(4-Gas-phenyl)-benzimidazole _; ι_基卜 'Methyl-pentanoic acid cyclohexylamine 2.1 Gas benzoic acid (43.8 mg, 0.28 mmol, 1.1 eq.) was added to 3-methylbutyron (21.5 mg, 0.38 mmol, 1.5 eq.), iso-cyanocyanine (30·6 mg, 0.28 mmob, 1.1 eq.) and a solution of N-t-butoxycarbonylphenylenediamine (52.1 mg, 0.25 mmol, 1 eq.) in methanol (5 mL). The reaction mixture was taken in a focused microwave (CEM Discovery) at 1 〇. The mixture was heated under stirring for 10 minutes. The solvent was removed in vacuo and the residue was redissolved in dichloromethane (2 mL). </RTI> </RTI> <RTI ID=0.0></RTI> </RTI> <RTI ID=0.0></RTI> <RTIgt; </RTI> <RTIgt; Butyl)-amino]-phenyl}-aminocarboxylic acid tert-butyl ester, 83 mg (61%). MS (ES+): 564 (M+H). 2.2 Concentrated HCl (25°/〇 in water, 〇.5 mL) was added to the crude {2-[(4-chloro-benzylidene H1-cyclohexylaminecarbazinyl) a solution of _methyl-butyl)-amino]-phenyl}-aminocarboxylic acid tert-butyl ester (83 mg, 0.12 mmol) in methanol (2.0 mL). Heating at 145 ° C for 3 minutes with stirring. The reaction mixture was subsequently evaporated and purified by preparative HPLC (gradient elution: water with 0.1% trifluoroacetic acid / acetonitrile) from 121967.doc -75 - 200811112 and under vacuum Evaporation. Then it was redissolved in di-methane (2 mL), PS-carbonate resin (4 mmol/g, 100 mg) was added and the mixture was shaken for 2 hours. The mixture was filtered and evaporated to give a white solid. 2-[2-(4-Chloro-phenyl)-benzimidazol-1-yl]-4-methyl-pentanoic acid cyclohexyl decylamine, 30 mg (460/〇) 〇MS (ES + ) : 424 (M+H). Example 3 4-{1-[Cyclohexyl-(4-morpholin-4-yl-phenylaminecarbazyl)-methyl]-1H-benzimidazol-2-yl Benzoic acid oxime ester hydrochloride 3.1 Add 4-N-morphinylbenzimidonitrile (1〇9 mg, 0.58 mmol, 1.1 eq.) to p-benzene Monomethyl decanoate (95 mg, 0.53 mmol, 1.1 eq.), hexane hexane plate (81 mg, 0.72 mmol, 1.5 eq.) and N-t-butoxycarbophenylenediamine (100 mg, 0) • 4 8 mmol, 1 equivalent) in the 'liquid of methanol' (ι·〇mL). The reaction mixture was heated in a focused microwave (CEM Discovery) at 100 C with stirring for 1 min. The solvent was removed in vacuo and the residue was crystallised m m m m m m m m m m m m m m m m m m m m m m m m m m m m m m m m m m m m m m m m m m m m m m m m m m m m m m evaporation. The crude product was purified by preparative HPLC (gradient elution: water with 0.1% trifluoroacetic acid / acetonitrile) and evaporated in vacuo to afford &lt;RTI ID=0.0&gt; Cyclohexyl _(4_Merline _4_ yl-phenylamine carbhydryl)-methyl]-terephthalate, 158 mg (49%). Ms (ES + ) : 671 (M+H). 3.2 121967.doc -76- 200811112 Concentrated HC1 (25% in water, 0.5 mL) was added to the crude {2-[(4_chloro-benzylidene H1-cyclohexylaminecarboxyl-3-methyl-) A solution of butyl)-amino]-phenyl-p-aminocarbamic acid tert-butyl ester (83 mg, 0.12 mmol) in methanol (2.0 mL). The reaction mixture was heated in a focused microwave (CEM Discovery) at 145 ° C for 3 minutes with stirring. The reaction mixture was evaporated, purified by preparative EtOAc (EtOAc: EtOAc (EtOAc) -4_yl-phenylamine-mercapto)-methyl]1H-benzimidazol-2-yl}-benzoic acid methyl ester hydrochloride, 78 mg (60%). MS (ES+): 553 (M+H). Example 4 2,N-Dicyclohexyl-2_[5,6-diox-2-(2,4-dimethoxy-phenyl)-benzoimin-1-ylpropiamine 4.1 in 〇 Di-tert-butyl dicarbonate (1.36 g, 6.21 mmol, 1β1 ▲) was added to 4,5-fluoro-benzene-l,2-diamine ( °·〇〇g, 5.65) at °C Ment, 1·〇 equivalent) in a stirred solution of tetrahydrofuran (10 mL) and N,N-diisopropylethylamine (0·81 g, 6.2 mmol, ι·ι), and the reaction mixture Stir for 16 hours and allow to warm to room temperature. The reaction mixture was evaporated in vacuo and the crude material was dried <RTI ID=0.0></RTI> </RTI> <RTI ID=0.0> (3_Amino-4,5-diox&quot;-phenyl)-tert-butylic acid tert-butyl ester, 〇·81 g (52〇/〇). MS (ES+) ·· 221,277 (Μ-tert-butyl, m+H). 4.2 Similar to Example 2· 1-2.2, benzoic acid, cyclohexane formaldehyde, isocyanide cyclohexane 121967.doc -77- 200811112 and (2-amino-4,5-dichloro-phenyl)-amine The third butyl carboxylic acid ester produces 2,N-dicyclohexyl-2_[5,6-dichloro-2-(2,4-dimethoxy-phenyl)-benzimidazole as a colorless oil. 1-yl]acetamide. MS (ES+): 544 (M+H). Example 5 2_Cyclohexyl-2-[2-(2,4.dimethoxy-phenyl)-benzimidazol-1-yl]-N-isopropyl-acetamide hydrochloride and examples Similar to 3-3.2, 2,4-dimethoxy-benzoic acid, cyclohexanecarboxylic acid, iso-isopropanyl isopropane and hydrazine-t-butoxycarbonylphenyldiamine give 2-cyclohexyl as a brown solid. 2_[2_(2,dimethoxy-phenyl>benzimidazole-yl]isopropyl-acetamide hydrochloride, ms (ES+): 436 (Μ+Η). Example 6 2, N-Dicyclohexyl_2_[octa(4-methoxyphenyl)benzimidazolylacetamide hydrochloride is similar to Examples 3.1-3.2, 4-methoxy-benzoic acid, cyclohexane Formaldehyde, isocyanocyclohexane and N_t-butoxycarbonylphenylenediamine give 2,N-dicyclohexyl 2 -[2-(4-decyloxy-phenyl)-benzene as a brown solid And imidazole_ι_yl]-acetamide hydrochloride, MS (ES + ): 446 (M+H). Example 7 2-cyclohexyl-2-[2-(3-methoxy-phenyl) - Benzopyrene 4_yl-bethylamine hydrochloride is similar to Example 3· 1-3.2, 3-methoxy-benzoic acid, cyclohexanefurfural, isocyanide cyclohexane and N·third Butoxycarbonylphenylenediamine produces 2 as a brown solid, Cyclohexyl-2- [2-(3-Methoxy-phenyl)-benzo.miso-1&gt;_yl]-acetamide hydrochloride, MS (ES+) ·· 446 (M+H). 121967.doc - 78 - 200811112 Example 8 2,N-Dicyclohexyl-2-[2-(2-methoxy-phenyl)-benzimidazole "- syl-acetamide hydrochloride is similar to Examples 3.1-3.2. 2-nonyloxy-benzoic acid, cyclohexanefurfural, isocyanocyclohexane and N-t-butoxycarbonylphenylenediamine give 2,N-cyclohexyl-2 in yellow oil. [2-(2-decyloxy-phenyl)-benzop-p-indole_ι_yl]-acetamide hydrochloride, MS (ES+): 446 (Μ+Η). Example 9 2,N- Dicyclohexyl-2-(2-naphthalen-1-yl-benzimidazol-1-yl)-acetamide hydrochloride is similar to Example 3 · 1 - 3 · 2, naphthalene-1-carboxylic acid, cyclohexane A jun, isocyanocyclohexane and N.3 butyloxycarbonyl phenylenediamine give a yellow oily 2, cycline-cyclohexyl-2-(2-naphthalen-1-yl-benzimidazole-1 -yl)-acetamide hydrochloride, MS(ES + ) : 466 (M+H) 〇 Example 10 2,N-Dicyclohexyl_2_[2_(3_ethoxy-phenyl)benzimidazole Small kibamine hydrochloride is similar to Examples 3.1-3, 2, 3-ethoxy-benzoic acid, cyclohexane carboxylic acid, Isocyanatocyclohexane and hydrazine-t-butoxy- thiophenylene diamine give 2, fluorene-dicyclohexyl-2-[2-(3-ethoxyphenyl)benzoic acid as a brown solid Saliva _ι_ kibamine hydrochloride, MS (ES + ) · · 460 (Μ + Η). Example 11 N. Cyclohexyl-2-[2-(2,4-dimethoxy-phenyl)-benzimidazolyl-4-phenyl-butanamine Similar to Example 28.3, 2,4-dimethyl Oxy-benzoic acid, 3-phenylpropanal, 121967.doc -79- 200811112 Isocyanatocyclohexane and 2-azido-phenylamine give N_cyclohexyl_2_[2·(2,4_ Dimethoxy-phenyl)-benzimidazole+yl]_4-phenylbutamine, ms (ES+): 498 (M+H) 〇 Example 12 N-cyclohexyl·2-[2-(2 , 4_dimethoxy-phenyl)·benzimidazolyl-3-methyl-butanamine hydrochloride is similar to Example 11-3.2, 2,4-dimethoxy-benzoic acid, 2-A Propionaldehyde, isocyanocyclohexane and N-t-butoxycarbonylphenylenediamine give N-cyclohexyl-2-[2-(2,4-dimethoxyphenyl)_ as a brown solid Benzimidazolyl-3-methyl-butanamine hydrochloride, ms (ES+): 436 (Μ+Η). Example 13 N-Cyclohexyl-2-[2-(2,4-dimethoxy-phenyl-benzimidazole β1- phenylpyrphenyl-propionamide hydrochloride is similar to Example 3· 1-3.2 , 2,4-dimethoxy-benzoic acid, phenylacetaldehyde, isocyanocyclohexane and N-t-butoxycarbonylphenylenediamine give N-cyclohexyl-2- as a milky white solid. 2-(2,4-Dimethoxy-phenyl)-benzimidazole]-yl] 3-phenyl-propanamide hydrochloride, MS (ES+): 484 (M+H). 14 N-Cyclohexyl-2-[2-(2,4-dimethoxy-phenylbenzimidazolyl)·octabitidine-2-yl-acetamide hydrochloride and examples 3· 1-3.2 Similarly, 2,4-dimethoxy-benzoic acid, pyridine-2-carboxylic acid, iso-cyanylcyclohexane and N-t-butoxycarbonylphenylenediamine give N-cyclohexyl as a brown oil. 2-[2_(2,4-Dimethoxy-phenyl)-benzimidazole-l-pyridin-2-yl-acetamide hydrochloride, MS (ESI): 471 (M+H). 121967.doc -80- 200811112 Example 15 N-cyclohexyl-2_cyclopentyl-2-[2-(2,4-dimethoxy-phenyl)-benzopyrene | The acid salt is similar to the examples 3.1-3.2, 2,4-dimethoxy-benzoic acid, cyclopentylformaldehyde, isocyanocyclohexane and N-third Oxycarbonyl phenylenediamine produces N-cyclohexyl-2-cyclopentyl 2 -[2_(2,dimethoxydiphenyl)benzimidazoles]-acetamide hydrochloride in a green solid Salt, MS (ES+): 462 (M+H). Example 16 4-{[1-cyclohexyl-(cyclohexylaminecarbazyl-methyl)]-1Η-benzimidazole_2_yl}-benzoic acid The methyl ester is similar to the examples 2.1-2.2. Monomethyl terephthalate, cyclohexanecarboxaldehyde, isocyanide cyclohexane and hydrazine-t-butoxycarbonylphenyldiamine give a white solid '{[1- Methyl cyclohexyl-(cyclohexylaminecarbazyl-methyl)]_1Η_benzimidazole_2_yl}-benzoic acid, MS (ES+): 474 (Μ+Η). Example 17 2,N-bicyclic Hexyl-2-(2-naphthalen-2-yl-benzimidazol-1-yl)-acetamide is similar to Examples 2.1-2.2, naphthalene-2-carboxylic acid, cyclohexanecarbaldehyde, isocyanide cyclohexane and N-tert-butoxycarbonylphenylenediamine produces 2,N_: bad hexyl-2-(2-qin-2-yl-benzoxanthene-1-yl)-ethonamide,]\ ^§(^|§+)· 466 (M+H). Example 18 2,N-Dicyclohexyl-2-[2-(3-thiophen-2-yl-phenyl)-benzimidazolyl] Acetamide is similar to the example 2 · 1 - 2 · 2 ' 3 -σ-cephen-2-yl- Formic acid, cyclohexene burnt 121967.doc -81 - 200811112 Disc, isocyanocyclohexane and N-t-butoxycarbonylphenylenediamine give 2,N-dicyclohexyl-2-[2] as a white solid -(3-Thien-2-yl-phenyl)-benzimidazol-1-yl]-acetamide hydrochloride, MS (ESI): 498 (M+H). Example 19 2,N-Dicyclohexyl-2-[2-(5-phenyl-thiophen-2-yl)-benzimidazolyl-1 yl acetamide is similar to Example 2.1-2-2, 5- Phenyl porphin-2-carboxylic acid, cyclohexane carboxylic acid, isocyanocyclohexane and N-tert-butoxycarbonyl phenylenediamine give 2,N-dicyclohexyl-2-[2] as a white solid -(5-phenyl-thiophen-2-yl)-benzimidazole-;μ-yl]-acetamide, MS (ES + ) : 498 (M+H) 〇 Example 20 3-{[1-cyclohexyl -(cyclohexylaminecarboxamyl-methyl)]_1H_benzimidazole_2_yl}-benzoic acid methyl ester is similar to the example 2· 1-2.2, monodecyl isophthalate, cyclohexanic acid, Isocyanation of cyclohexane and N-t-butoxycarbonylphenylenediamine to give 3-{[1-cyclohexyl-(cyclohexylamine fluorenyl-fluorenyl benzoate wow_2_yl} as a white solid - Benzyl benzoate, MS (ES+): 474 (M+H). Example 21 2-[2-(3-hydroxy-phenyl)-benzimidazol-1-yl]- 4-methyl-pentanoic acid Hexylamine is similar to Example 2·1-2.2, 3-hydroxybenzoic acid, 3-methylbutyridine, iso-nitriding cyclohexane and hydrazine-t-butoxycarbonylphenyldiamine are produced as a white solid. 2-[2-(3-Hydroxy-phenyl)-benzimidazol-1-yl]-4-methyl- Acid cyclohexylamine, MS (ES + ) : 406 (M+H) 〇 Example 22 121967.doc -82- 200811112 2-[2-(4-Hydroxymethyl-phenyl)-benzimidazole-1- 4-methyl-pentanoic acid cyclohexylamine is similar to the example 2_1-2-2, 4-hydroxymercaptobenzoic acid, 3-mercaptobutyl, isocyanocyclohexane and anthracene-tert-butoxycarbonyl Phenylenediamine gives 2-[2-(4-hydroxymethyl-phenyl)-benzimidazol-1-yl]-4-methyl-pentanoic acid cyclohexylamine as a white solid, MS (ES+): 420 (M+H). Example 23 2-[2-(1Η-吲哚-5-yl)-benzimidazol-1-yl-4-methyl-pentanoic acid cyclohexyl decylamine similar to Example 2.1-2.2 , 1H-吲哚_5_carboxylic acid, 3-methylbutyl, isocyanocyclohexane and N-t-butoxycarbonylphenylenediamine give 2-[2-(1Η-吲哚) as a white solid -5-yl)-benzimidazol-1-yl]-4-methyl-pentanoic acid cyclohexyl decylamine, MS (ES + ): 429 (M+H). Example 24 2·[2_(1Η-吲哚-6-yl)-benzimidazole-1-yl]-4-methyl-pentanoic acid cyclohexyl decylamine is similar to the examples 2.1-2.2, 1Η-吲哚-6-carboxylic acid, 3-methyl-butyl, Isocyanatocyclohexane and hydrazine-t-butoxycarbonylphenylenediamine produce 2_[2-( 111-Azepine-6-yl)-benzoimin-1-yl]-4-methyl-pentanoic acid cyclohexyl hydrazine hydrochloride, MS (ES + ): 429 (Μ + Η). Example 25 2 [2-(4-Amino-benyl)-existing oxime-based 4-methyl-pentanoic acid cyclohexylamine is similar to Example 2·1-2.2, 4-aminobenzoic acid, 3 -methylbutyraldehyde, isocyanocyclohexane and N-tert-butoxycarbonylphenylenediamine are produced as a white solid 2_ 121967.doc -83 - 200811112 [2-(4-Amino-phenyl)- Benzimidazol-1-yl]-4-methyl-pentanoic acid cyclohexyl decylamine hydrochloride, MS (ES+): 405 (M+H). Example 26 2_Cyclohexyl-2-[2-(2,4-dioxalyl-phenyl)-stupid odor-yl] ((R)l-phenyl-ethyl)-acetamide Example 2.1-2-2 is similar, 2,4-dimethoxy-benzoic acid, cyclohexanalfurfural, (1-isocyano-ethyl)-benzene and hydrazine-tert-butoxycarbonylphenyldiamine Produces 2-cyclohexyl-2-[2-(2,4-dimethoxy-phenyl)-benzoxyl-1 -yl]-N-((R) 1-phenyl- as a white solid Ethyl)-ethylamine, VIS (ES + ): 498 (M+H). Example 27 2,N-Dicyclohexyl-2-[2·(4-hydroxymethyl-phenyl)-benzimidazole·1yl]-acetamide Similar to Example 2.1-2.2, 4-hydroxymethylbenzene Formic acid, cyclohexanefurfural, isocyanocyclohexane and hydrazine-t-butoxycarbonylphenylenediamine give a white solid 2, fluorene-dicyclohexyl-2-[2-(4-hydroxymethyl) -Phenyl)-benzimidazol-1-yl]-acetamide, MS (ES+): 446 (Μ+Η). Example 28 N-cyclohexyl-2-[2.(2,3.dimethoxy-phenyl)-benzimidazol-1-yl]-4-phenyl-butanamine 28.1 at 〇 ° C, The o-aminobenzoic acid (12.3 g, 90 mmol) was dissolved in a mixture of aqueous HCl (36%, 50 mL), H20 (100 mL), dioxane (50 mL) and methanol (50 mL) and dissolved 121967.doc -84- 200811112 in H2O (50 ml)

NaN02 (7.6 g, 110 mm〇l) was treated dropwise, while the temperature of the reaction mixture was kept below. After 1 hour, the mixture was poured into an ice-cold solution of sodium acetate (26 g, 317 mmol) and sodium azide (15 g, 23 〇 mm 〇 1) in about 300 ml of water. The resulting suspension was extracted with EtOAc (~3×), and combined organic phases were evaporated and evaporated. MS (ES+): 164 (M+H). 28.2 2_Azido-benzoic acid (3.7 g, 22.7 mmol) in dimethylformamide (75 mL) was cooled to -10 °C and ethyl chloroformate (2·6 g, 24) Mm〇1) Processing. After stirring for 1 hour at -1 (TC), NaN3 (7.28 g, 112 mmol) dissolved in h2 〇 (5 〇mL) was added and the mixture was allowed to reach ambient temperature. H 2 〇 (3 00 ml) was added and the mixture was used. The ethyl acetate phase was extracted three times. The ethyl acetate phase was dried over Na 2 SO 4 and stirred at ambient temperature for 96 hours. The formed precipitate was filtered and subjected to Si〇 2 chromatography using ethyl acetate/hexane as a solvent. Yield 304 mg (19%) of 2-azido-phenylamine. MS (ES+): 135 (M+H) 〇28.3 2- 2-indoleylphenylamine (68 mg, 0.5 mmol), 2,3 a mixture of dimethoxybenzoic acid (91 mg, 0.5 mmol), 3-phenylpropanal (67 mg, 0.5 mmol), isocyanated hexanone (55 mg '0.5 mmol) in 2 ml of methanol Stir at room temperature for 64 hours. The mixture was diluted with 7 ml of methane and treated with 25 μM of diisopropylethylamine. After cooling to 〇 ° C, 450 mg of polymer-bound diphenylphosphine (SP_15002B154) was added. , 3 mmol/g) and the mixture was allowed to reach room temperature within 5 hours. The resin was then filtered off, washed with a methylene gas and stirred in toluene at 121967.doc -85 - 200811112 100 ° C for 8 hours. Filter shift Resin and evaporation of the solvent gave 70 mg (28%) of N-cyclohexyl-2-[2-(2,3-dimethoxy-phenyl)-benzimidazole. Phenyl-butanin, MS (ES+): 498 (M+H). Example 29 2- [2-(3-Cyano-phenyl)-benzimid-1-yl]-2,N- Dicyclohexyl-acetamide is similar to Example 2· 1-2.2, 3-cyanobenzoic acid, cyclohexanecarboxaldehyde, isocyanocyclohexane and N-tert-butoxycarbonylphenylenediamine give a white solid 2_ [2 - (3 - gas-based)-benzine. Rice bran sits -1 _yl]· 2,N-di- cumyl-ethylamine, MS (ES + ) : 441 (Μ+Η 〇Example 30 2,~Dicyclohexyl-2-{2-[4-(111_tetraindole-5-yl)-phenyl]-benzoxan-1-yl}•acetamide hydrochloride Similar to Examples 3.1-3.2, 4·(1Η-tetras-5-yl)-benzoic acid, cyclohexane-formaldehyde, isocyanatocyclohexane and hydrazine-t-butoxycarbonylphenylenediamine were produced in milky white. Solid 2, Ν-dicyclohexyl-2-{2_[4-(1Η-tetrazol-5-yl)-phenyl]-benzimidazol-1-ylbutylidene hydrochloride, MS (ES + ) : 484 (Μ+Η). Example 31 3- [1-(Benzylaminoindenyl-cyclopentyl-methyl-methyl 1H-benzimidazolylphthalic acid) The methyl ester was similar to Example 2·1 - 2.2, 3-methoxycarbonyl-benzoic acid, cyclopentanecarboxylic acid, isocyanobenzyl and N-t-butoxycarbonylphenylenediamine gave a white solid. -[1-(Benzylaminocarbamimidyl-cyclopentyl-methyl)_1H_benzimidazole-2-yl]-benzoic acid methyl ester, MS (ESI+): 468 (M+H). 121967.doc -86- 200811112 Example 32

Cyclohexyl decyl hexanoate, MS -1-yl]-hexanoic acid cyclohexyl decylamine, 2,3-methoxy-benzoic acid, amyl, isocyano-phenylamine to give 2-[2-( 2,4-Dimethoxy-phenyl)_ (ES+): 450 (M+H). Example 33 2'N-Dicyclohexyl_2_[2♦ methanesulfonyl-phenyl)benzimidazole small group] Ethylamine hydrochloride is similar to Example 3·1-3.2, 3_methanesulfonyl _ Benzoic acid, cyclohexanemethyl, isocyanocyclohexane and glacial tert-butoxycarbonylphenylenediamine give 2,N-dicyclohexyl_2-[2_(3_methanesulfonyl) as a brown solid -Phenyl)-benzimidazole- 1 -yl]-acetamide hydrochloride, MS (ES+): 494 (M+H). Example 34 N-Benzyl-2-cyclohexyl-2-[2·(2,4-dimethoxy-phenyl-benzimidazolyl)-acetamide is similar to Example 2· 1-2.2, 2 , 4-dimethoxy-benzoic acid, cyclohexanecarboxylic acid, isocyanobenzylidene and anthracene-t-butoxy phenyldiamine give yttrium-benzoin-2- as a yellow oil Cyclohexyl-2-[2-(2,4-dimethoxy-phenyl)-benzimidazolyl-1-ylethaneamine, MS (ES+): 484 (Μ+Η). Example 35 2- Cyclohexyl-2-[2-(2,4-dimethoxy-phenyl)-benzimidazole_1β-yl]-]&gt;Ηι·methyl-butyl)-acetamide and Example 2·1 -2.2 similar, 2,4-dimethoxy-benzoic acid, cyclohexane methyl 121967.doc -87- 200811112 Jun, 2-isocyanopentane and N-third butoxy-phenylenediamine production 2-Cyclohexyl-2-[2·(2,4-dimethoxy-phenyl)-benzimidazole-yl]-indole-(1-methyl-butyl)-acetamidine as an orange solid Amine, MS (ES+): 464 (Μ+Η). Example 3 6 4-[1-(Benzylaminocarbamimido-cyclopentyl-methyl)_1H_benzimidazol-2-ylbenzoic acid oxime ester is similar to Example 2·1-2.2, 4-A Oxycarbonyl-benzoic acid, cyclopentane-methyl, isocyanobenzyl and N-tert-butoxycarbonylphenylenediamine give 4-[1-(benzylaminocarbamyl) as a white solid. Cyclopentyl-methyl)benzo benzoyl-2-yl]-benzoic acid methyl ester, MS (ES+): 468 (M+H). Example 37 N-Cyclopentyl-2-[2-(3-methoxy-phenyl)-benzoindolyl-4-phenyl-butanamine hydrochloride is similar to Examples 3.1-3.2, 3- Methoxy-benzoic acid, 3-phenylpropanal, isocyanocyclopentane and N-t-butoxycarbonylphenylenediamine give a pentyl-2-[2-(3-oxo) group as a brown solid Benzyl-phenyl)-benzopyrene _1_1_yl]_4·phenyl-butanamine hydrochloride, MS (ES+): 454 (Μ+Η). Example 38 2,N-Dicyclohexyl_2-[2-(2,4-dimethoxyphenyl)-5-methyl-benzimidazole-1-yl]-acetamide hydrochloride and examples Similar to 3-3.2, 2,4-dimethoxy-benzoic acid, cyclohexane-burning formic acid, isocyanocyclohexane and N-tert-butoxycarbonyl 5-methylphenylenediamine give a white solid 2,N-Dicyclohexyl-2-indole (2,4-dimethoxy-phenyl)-5-methyl-benzimidazole-buyl]-acetamide hydrochloride, MS (ES+): 490 121967.doc -88- 200811112 (M+H) 〇Example 39 2-[2-(heart phenyl)-benzimidazole + yl] _2, dicyclopentyl pentylamine hydrochloride and Example 3.1 Similar to -3.2, 4-chloro-benzoic acid, cyclopentane formaldehyde, isocyanatocyclopentane and N-t-butoxycarbonylphenylenediamine gave 2-[2_(4-chloro-phenyl) as a white solid. -benzimidazole-i-yl]-2,N-dicyclopentyl-acetamide hydrochloride, MS (ES+): 422 (M+H). Example 40 N-Diphenylmethyl-2-cyclohexyl-2-[2-(2,4-dimethoxy-phenyl)-benzimidazole-1-yl]-ethanoamine and Example 2·1 -2.2 Similarly, 2,4-dimethoxy-benzoic acid, cyclohexanecarboxaldehyde, isocyanobenzene diphenylmethane and N-tert-butoxycarbonylphenylenediamine give N-benzophenone as a brown solid Benzyl-2-cyclohexyl-2·[2-(2,4·dimethoxy-phenyl)·benzoquinone-1-yl]ethenylamine, MS (ES+) : 560 (Μ+Η) . Example 41 N-Benzyl- 2_(2-Cate-1-yl-benzopyran-1-yl)-4-phenyl-butylamine Similar to Example 2·1-2·2, naphthalene-1 - formic acid, 3-phenylpropanal, isocyanoquinone and hydrazine-t-butoxycarbonylphenylenediamine give a white solid Ν-benzyl-2-(2-naphthalenyl-1-yl) Benzoin-1-yl)-4-phenyl-butanamine, ms (ES + ): 496 (M+H). Example 42 2-Cyclohexyl-2_[2_(2,4-dimethoxy-phenyl)·benzimidazole·[_yl]_N-('methoxy-phenyl)-acetamide 121967. Doc -89- 200811112 Similar to Example 2.1-2.2, 2, 'dimethoxybenzoic acid, cyclohexanefurfural, isocyanatocardiylphenyl and N_t-butoxycarbonylphenylenediamine 2·cyclohexyl-2-[2-(2,4-dimethoxy-phenyl)-benzimidazol-1-yl]-N-(4-methoxy-phenyl) as a color oil Ethylamine, ms (ES+) ·· 5 00 (M+H) 〇 Example 43 2,N-Dicyclohexyl_2_[2-(2,4-dimethoxy-phenyl)_4_A The base-benzimidazole-l-yl]-ethyl amide is similar to the examples 2· 1-2.2, 2,4-dimethoxy-benzoic acid, cyclohexanecarboxylic acid, isocyanocyclohexane and N- Third butoxycarbonyl 6-methylphenylenediamine produces 2,N-dicyclohexyl-2-indole (2,4-dimethoxy-phenyl)-4-methyl-benzimidazole as a brown solid Small base]_acetamide, MS (ES + ): 490 (M+H). Example 44 2,N--Cyclohexyl_2_ {2-[3-(2-Sideoxy- ηbiprozin-1-yl)-phenyl]-benzimidazol-1-ylethylamine salt The acid salt is similar to the examples 3.1-3.2, 3-(2-o-oxy-pyrrolidin-1-yl)-benzoic acid, cyclohexanecarboxaldehyde, isocyanocyclohexane and N-tert-butoxycarbonylbenzene The diamine produces 2,N-dicyclohexyl-2-{2-[3-(2. oxo-pyrrolidin-1-yl)-phenyl]-benzimidazole-bukib Indole hydrochloride, MS (ES+): 499 (M+H). Example 45 2,N-Dicyclohexyl·2-[2-(2-o-oxy-1,2-dihydro-pyridyl)·benzimid-1-yl]-ethenylamine and Example 2.1 _2 .2 similar, 2-methoxy-isonicotinic acid, cyclohexane formaldehyde, iso 121967.doc •90· 200811112 cyanide cyclohexane and N-t-butoxycarbonylphenyldiamine in the accompanying 2-methoxy Partially hydrolyzed to a 2-sided oxy group, 1,2-dihydrogen 111, which produces a milky white solid in the process of biting the base, 2, Ν-dicyclohexyl_2_[2_(2_ side Oxy _ 1,2-di-r-butyryl-4-yl)-benzoquinone-l-yl]-ethanoamine, ms (ES + ): 433 (M+H). Example 46 N-Cyclopentyl-2-[2-(2-methoxy-phenyl)-benzofurazyl 4-phenyl-butanamine Similar to Examples 2.1-2.2, 2-methoxy Benzoic acid, 3-phenylpropanal, iso-gasified cyclopentane and hydrazine·t-butoxy phenyldiamine give a white solid Ν-cyclopentyl_2-[2-(2-曱) Oxy-phenyl)·benzimidazole-indole-yl]_4_phenyl-butanamine, MS (ES+): 454 (Μ+Η) 〇 Example 47 2-cyclohexyl-2-[2·(2 , 4-dimethoxy-phenyl)-benzopyrimidin-l-butyl...pentyl-acetamide is similar to Example 2·1-2.2, 2,4-dimethoxy-benzoic acid, cyclohexyl Pyrophoric acid, isopentane pentane and hydrazine-t-butoxycarbonylphenyldiamine give 2-cyclohexyl-2-[2-(2,4-dimethoxy-phenyl)_ as a white solid Benzimidazol-1β-yl]·Ν-pentyl-acetamide, MS (ES+): 464 (Μ+Η). Example 48 N-Benzyl-2·[2-(4-Gas-phenyl)-benzimidazole_1-ylpy-2-cyclopentyl-acetamide hydrochloride was similar to Example 3.1-3.2, 4 -Chlorobenzoic acid, cyclopentanecarboxaldehyde, isocyanobenzenemethyl and N-tert-butoxycarbonylphenylenediamine to produce ice benzene as a brown solid 121967.doc -91- 200811112 methyl-2-[2- (4-Gas-phenyl)-benzimidazole _ 丨-yl]_2-cyclopentyl-acetamide hydrochloride, MS (ES+): 444 (M+H) 〇 Example 49 2, dicyclopentane 2-(2-naphthalen-1-yl-benzoxanthene-1)-glyoxime is similar to Example 2·1-2.2, naphthoic acid, cyclopentane formaldehyde, isocyanocyclopentane and N -T-butoxycarbonylphenylenediamine produces 2,N_:cyclopentyl·2-(2-naphthalen-1-yl-benzopyrene+yl)-acetamide, ms (ES+) as a white solid. : 438 (M+H). Example 50 2_[2·(3-Cyano-phenyl)-benzimidazole_1-ylbu-N-cyclohexyl-4-phenyl-butanamine is similar to Example 28.3. 3-cyanobenzoic acid, 3-phenylpropanal, isocyanocyclohexane and 2-azido-phenylamine give 2_[2_(3-cyano-phenyl)-benzimid-1 -yl]cyclohexyl-4_phenyl-butanamine, Ms (ES+): 463 (M+H) 〇 Example 51 2-[2-(4-hydroxy- Benzo-benzimidazole-1β-based fluorenyl-pentanoic acid cyclohexyl decylamine hydrochloride is similar to the examples 3.1-3.2, 4-hydroxybenzoic acid, 3-methylbutanal, isocyanatocyclohexane And hydrazine-t-butoxycarbonylphenylenediamine produces 2_[2_(4-hydroxy-phenyl)-benzimidazole_丨_基卜4_mercapto-pentanoic acid cyclohexyl decylamine hydrochloride as a brown solid Salt, MS (ES+): 406 (M+H). Example 52 N-tert-butyl-2·cyclohexyl-2-[2-(2,4-dimethoxy-phenyl)-benzimidazole A 121967.doc -92- 200811112 1-yl]-acetamide is similar to the examples 2.1-2.2 '2,4-dimethoxy-benzoic acid, cyclohexane-formaldehyde, isocyanated tert-butyl and N- Third butoxycarbonylphenylenediamine produces N-tert-butyl-2-cyclohexyl·2-[2-(2,4-dimethoxy-phenyl)-benzimidazole-1 as a white solid -yl]-acetamide, MS (ES+): 450 (Μ + Η). Example 53 4-[1-(1-phenylhydrazinocarbazinyl-3-phenyl-propylidene 1H-benzo Imidazolyl-2-yl]methyl Benzoate is similar to Example 2· 1-2.2, monomethyl terephthalate, 3-phenylpropanal, isocyanobenzyl and N-tert-butoxycarbonyl Phenylenediamine produces 4-[1-(1-Benzyl) as a white solid Yue acyl amine _3- phenyl - propyl) benzimidazol-_111_ _2_ yl] methyl Yue _ benzene, MS (ES +): 504 (M + H). Example 54 Methyl cyclohexylamine-methylindolyl-3-phenyl-propyl)-111-benzimidazol-2-yl]-benzoate similar to Example 28.3, monomethyl terephthalate, 3-phenyl Propionaldehyde, isocyanocyclohexane and 2-azido-phenylamine give benzylamine carbazino-3-phenyl-propyl)-1 quinone-benzimidazol-2-yl as a brown solid ]-Phenyl benzoate, MS (ES+): 496 (M+H). Example 55 2,N-Dicyclopentyl-2-[2-(2-methoxy-phenyl)-benzimidazol-4-yl]-acetamide Similar to Example 2.1-2.2, 2-methoxy Benzoic acid, cyclopentane formaldehyde, isocyanatocyclopentane and N-tert-butoxycarbonylphenylenediamine give a creamy solid 2, Ν·dicyclopentyl 2–[2-(2- Methoxy-phenyl)-benzimidazole-1-yl]-B 121967.doc -93- 200811112 decylamine, MS (ES+): 418 (M+H). Example 56 2,N-Dicyclohexyl-2-[2-(2,4-dimethoxy-phenyl)-naphtho[2,3-d]imidazolium-1-yl]-acetamide and Example 2 Similar to 1-2.2, 2,4-dimethoxy-benzoic acid, cyclohexane-burning formic acid, isocyanocyclohexane and (3-amino-naphthalen-2-yl)-carbamic acid tert-butyl vinegar 2,N-Dicyclohexyl-2-[2-(2,4-dimethoxy-phenyl)-naphtho[2,3-d]m-butan-1-yl]-B as a yellow solid Indoleamine, MS (ES+): 526 (M+H) 〇 Example 57 2- [2-(2,3-Dimethoxy-phenyl)-benzimidazole-1 yl-4-methyl-pentyl The acid cyclohexylamine is similar to the example 28.3, 2,3-dimethoxybenzoic acid, 3-methylbutanal, isocyanocyclohexane and 2-azido-phenylamine give 2-[2_( 2,3-Dimethoxy-phenyl)-benzimidazol-1-yl]-4-methyl-pentanoic acid cyclohexylguanamine, MS (ES+): 450 (M+H). Example 58 N-Benzyl-2-[2-(2-methoxy-phenyl)-benzopyridin-1-yl]-4-phenyl-butanamine is similar to Example 2.1 _2. 2-methoxybenzoic acid, 3-phenylpropanal, isocyanobenzyl and hydrazine-t-butoxycarbonylphenylenediamine give a white solid Ν-benzyl-2-[2-( 2-methoxy-phenyl)-benzimidazole small group]-4-indolyl-butanamine, MS (ES + ) ··476 (Μ+Η). Example 59 121967.doc -94- 200811112 2-Cyclohexyl-2-[2_(2,4-dimethoxy-phenyl)-benzoxanthene+yl]-N_(3_isopropoxy-propyl )-acetamide is similar to the example 2.U.2, 2,4-dimethoxybenzoic acid, cyclohexane formaldehyde, 1-isocyano-3-isopropoxy-propane and N_third Butoxycarbonylphenylenediamine produces 2-cyclohexyl[2-(2,4-dimethoxy-phenyl)-benzomidine-1-yl]-N-(3- Isopropoxy-propyl)-acetamide 'MS (ES+): 494 (M+H). Example 60 2-[2-(2,4-Dimethoxy-phenyl)-benzimidazol-1-ylbu]^isopropyl-4-ylphenyl-butanamine is similar to Example 28.3, 2, 4-Dimethoxyoxybenzoic acid, 3-phenylpropanal, isocyanopropylidene and 2-azido-phenylamine give 2-[2-(2,4-dimethoxy-phenyl) - benzo-benzo-1-yl]-N-isopropyl-4-phenyl-butanamine, Ms (ES + ): 458 (M+H). Example 61 N-Benzyl-2-cyclodecyl-2-(2-naphthalen-1-yl-benzimidazole 4 yl)-acetamide is similar to Example 2·1-2.2, naphthalene-1-anthracene Acid, cyclopentanyl, isocyanatomethyl and N-di-dibutoxy-a basic amine produces N-benzyl-2-cyclopentyl-2-(2•naphthalene) as a white solid -1·Bis-benzimidazole-1-yl)-acetamide, ms (ES+): 460 (M+H). Example 62 2,N-Dicyclohexyl·2-[2-(2,3-didecyloxy-phenyl)- benzopyridinyl]-acetamide is similar to Example 28.3, 2,3-di Methoxybenzoic acid, cyclohexanic acid, 121967.doc •95- 200811112 Isocyanatocyclohexane and 2-azido-phenylamine give 2, indane dicyclohexyl_2_[2_ (2,3- Monomethoxy-phenyl)-benzimidazolyl]-acetamide, ms (es+): 476 (M+H). Example 63 2-[2-(2,4-Methoxy-phenyl)-benzimidazole β1_yl]_4_methyl-pentanoic acid Cyclohexyl decylamine

Similar to Example 28.3, 2,4-dimethoxybenzoic acid, 3-methylbutanal, isocyanocyclohexane and 2-azido-phenylamine yield 2_[2-(2,4-di) Methoxy-phenyl)-benzimidazole-l-yl]methyl-pentanoic acid cyclohexyl decylamine, MS (ES + ) : 450 (M+H) 〇 Example 64 2-cyclohexyl-2-[2_ (2,3-dimethoxy-phenyl)-benzimidazole 4·kib N•isopropyl-acetamide

Similar to Example 28·3, 2,3-dimethoxybenzoic acid, cyclohexanone, iso-isocyanide and 2-azido-phenylamine yield 2-cyclohexyl_2_[2_(2 , 3_monomethoxy-stupyl)-benzimidin-1-yl]isopropyl-acetamide, MS (ES + ) ·· 436 (M+H). Example 65 - 卩-^-dimethoxy-phenyl-benzimidazole-^ kib &amp; isopropyl-p-phenyl-butanamine Similar to Example 28.3, 2,3-dimethoxy Benzoic acid, % phenylpropanal, isopropane isopropane and 2-azido-phenylamine give 2_[2 gas 2, bis-dimethoxy-phenyl)-benzimidazole-i-yl]_N_ Isopropyl_4_phenyl.butanamine, ms (ES+): 458 (M+H) 〇121967.doc -96- 200811112 Example 66 2 ringing [2·(4-ethyl&quot;&quot;phenyl Benzene-salt-small-base N-cyclohexyl-4-phenylbutyramine is similar to Example 28.3, 2,4-ethlylbenzoic acid, 3-phenylpropanal, isopropylidene-hexane Azido-phenylamine produces 2-[2-(4-ethinyl-phenyl)-benzimidazol-1-yl]cyclohexylphenyl-butanamine, ms (ES+): 480 (M+ H). Example 67 N-N-methyl-2-[2-(4-carbo-phenyl)-benzimidazolyl-p-phenyl-butanamine hydrochloride is similar to Example 3.1-3.2, 4-chlorobenzoic acid , 3-phenylpropanal, isocyanoquinone and hydrazine-t-butoxycarbonylphenylenediamine give a white solid... benzyl 2-[2-(4-chloro-phenyl)-benzene嗤 嗤 丨 基 基 ] ] 基 基 基 基 基 MS MS MS MS MS MS MS MS MS MS MS MS MS MS MS MS MS MS MS Example 68 4-[1-(1-Isopropylaminocarbazyl-pentyl)-1]3-benzimidazol-2-yl]-benzoic acid methyl ester Similar to Example 28.3, terephthalic acid single Methyl ester, valeraldehyde, isopropane isopropane and 2_azido-phenylamine give methyl ester of 'isopropylaminemethanyl-pentyl}_1 "benzimidazol-2-yl]-benzoate, MS (es+) ·· 4〇8 (M+H). Example 69 N-Butyl-2-[2-(2,4-dimethoxy-phenyl)-benzimidazole phenyl-acetamide 121967.doc -97· 200811112 Similar to Example 28.3, 2,4 -Dimethoxybenzoic acid, benzaldehyde, isocyanobutane and 2-azido-phenylamine to produce N-butyl-2 &lt;2_(2,4-dioxyl-phenyl)-benzimidazolyl]_2-phenyl-acetamide, MS (ES+): 444 (M+H). Example 70 2-[2-(2,3-Dimethoxy-phenyl-benzimidazolyl-4-yl-pentyl isopropyl decylamine is similar to Example 28.3, 2,3-dimethoxy Benzoic acid, 3-methylbutanal, isopropane isopropane and 2-azido-phenylamine give 2_[2_(2,3-dimethoxy-phenyl)-benzopyrene-丨_ base]·4•methyl-pentanoic acid isopropyl decylamine, ms (ES + ) : 410 (M+H) 〇 Example 71 2-Benzo[1,3]dioxolyl N_butyl_2_丨2_(2,3-dimethoxy-phenyl)-benzopyranyl]-acetamide is similar to Example 28·3, 2,3-dimethoxybenzoic acid, Benzo[1,3]dioxolane-5-carboxaldehyde, isocyanobutane and 2-azido-phenylamine give indolo[1,3]dioxole-5 -yl-N-butyl_2-[2-(2,3-dimethoxy-phenyl)-benzomidine. Sit-:^^^^^^^, Ms (ES+): 488 (m+ H). Example 72 2-Benzo[1,3]dioxole·5_base term _butyl_2_[2_(2,4-dimethoxy-phenyl)-benzoic Salivyl]-acetamide is similar to Example 28·3, 2,4-dimethoxybenzoic acid, benzo[1,3]dioxapentan-5-formaldehyde, isocyanobutane and 2· Azido-phenylamine 2·Benzo[1,3]-oxocyclopent-5-yl-N-butyl-2-[2·(2,3-dimethoxy_ 121967.doc -98- 200811112 phenyl )-benzimidazole small group]-acetamide, Ms (ES+): 488 (M+H). Example 73 N-butyl·2-[2-(2,4-dimethoxy-phenyl) Benzopyranyl] 2_(2_qi_phenyl)-acetamide is similar to Example 28.3, 2,4-dimethoxybenzoic acid, fluorobenzaldehyde, isocyanide, and 2 -璺N-phenyl-phenylamine produces Ν_butyl_2_[2_(2,4-dimethoxy-phenyl)-benzimidazole_;[_yl]_2_(2-fluoro-phenyl)_acetamidine Amine, Ms (ES+) · · 462 (M+H) 〇 Example 74 N-Cyclopentyl-2-[2-(3-hydroxy-phenyl)-benzimidazolyl-4-phenyl-butanamine Similar to κ, 2.1-2.2, 3-carbylbenzoic acid, 3-phenylpropenyl, isocyanato-pentyl and N-tert-butoxycarbonylphenylenediamine gave N-cyclopentyl 2 as a white solid. [2-(3-Carbo-phenyl)-benzopyrimidine-hydrazinyl]- 4-phenyl-butanamine hydrochloride, MS (ES+): 440 (M+H). (4 ethyl fluorenyl group) Benzene 嗤 嗤 ^ 基 基 基 与 与 与 与 与 与 与 与 与 与 与 与 与 与 与 与 与 与 与 与 与 与 与 与 与 与 与 与 与 与 与 与 与 与Alkane and 2-azido-phenylamine give 2_[2_ethinyl-phenyl)-benzimidazole _ bromo-isopropyl isopropyl decylamine, MS (ES+): 392 (M+H ). Example 76 N-Butyl·2_[2-(2,3-dimethoxy-phenyl&gt;benzimidazolyl]_2_phenyl-acetamidamine is similar to Example 28.3, 2,3-dimethoxy Benzoic acid, benzaldehyde, isocyanide 121967.doc -99- 200811112 Butane and 2-azido-phenylamine give N_butyl-2_[2_(2,3-dimethoxy) as a brown solid -phenyl)_benzimidazole_丨_yl]_2_phenyl-acetamide. MS (ES + ) : 444 (M+H) 〇 Example 77 2-[2_(4-Ethyl-phenyl Benzimidazolyl 4-methyl-pentanoic acid cyclohexyl decylamine is similar to Example 28.3 '4·Acetylbenzoic acid, 3-methylbutyric acid, isocyanocyclohexane and 2-azido- Phenylamine produces 2-[2-(4-ethinyl-phenyl)-benzoimin-1-yl]-4-methyl-pentanoic acid cyclohexyl decylamine, ms (ES + ) : 432 ( M+H). Example 78 N-butyl-2·[2-(2,3-dimethoxy-phenyl-benzimidazole β1-yl b 2 o-tolyl-acetamide) is similar to Example 28.3 ' 2,3-Dimethoxybenzoic acid, 2-methylphenyl hydrazine, terminally cyanidation, and 2-aza-nitro-phenylamine to produce Ν-butyl-2-[2-(2,3_ Dimethoxy-phenyl)-benzimidazol-1-yl]_2-o-tolyl-acetamide, MS (ES + ) : 458 (M+H) Example 79 & Butyl-2_[2-(2,3-dimethoxy-phenyl)-benzimidazolyl-1-yl]-2-(4-methoxy-phenyl)·acetamide Similar to Example 28.3, 2,3-dimethoxybenzoic acid, 4-methoxybenzaldehyde, isocyanobutane and 2-azido-phenylamine gave N_butyl_2_[2_(2 ,3_Dimethoxy-phenyl)-benzommethoxy-phenyl)-acetamide, MS (ES + ) : 474 (M+H). 121967.doc -100- 200811112 Example 80 N Base 2 [2 (2,3-methoxy-phenyl)-benzoxanthene]yl-phenyl)-acetamide is similar to Example 28.3 as '2,3-dimethoxybenzoic acid, 2-Fluorobenzoic acid, isobutyl cyanide and 2-azido-phenylamine give N-butyl_2_[2·(2,3.dimethoxy-phenyl)-benzoate. ·Buji]-^.Gas_phenyl)_Ethylamine, ms (ES+): 462 (M+H). Example 81 N-butyl-2,[2-(2,3-dimethoxyoxyphenyl)benzoyl-saltyl]2-(4-didecylamino-phenyl)-acetamidine The amine is similar to the example 28.3, 2,3-dimethoxybenzoic acid, dinaben, isocyanobutane and 2-azido-phenylamine give Ν _ butyl soil · 2 · [2' ( 2,3-monomethyl-phenyl)-benzoxazole+yl]_2_(4-dimethylamino-phenyl)-acetamide, MS (ES+): 487 (Μ+Η) . Example 82 2-[2-(2,3.Dimethoxy-phenyl)benzene(tetra)pyrene + isopropylamide of isopropylhexanoate similar to Example 2", 2,3-dimethoxybenzoic acid, Valeraldehyde, iso-isocyanide and 2-$nitro-phenylamine give 2_[2 &lt;2,3-Dimethoxy-phenyl) </RTI> </ RTI> </ RTI> </ RTI> </ RTI> <RTIgt; Example 83 4-{1_[(2-Fluorophenyl)-isopropylaminecarboxamyl_methyl]-Chloro-benzoxazole-2_ Benbbenzoic acid methyl ester Similar to Example 28.3, terephthalic acid Monomethyl G, 2_Fluorobenzaldehyde, Iso 121967.doc -101- 200811112 Oxidized isopropylidene and 2-azido-phenylamine to produce heart {1_[(2_gas-phenyl)_isopropyl Hydrazinyl-methyl HH-benzopyryltamidyl benzoic acid methyl ketone, (10) (ES+): 446 (M+H). Example 84 2-[2-(3-Cyano-phenyl)-benzimidazole small group] _4-methyl-pentanoic acid cyclohexyl decylamine is similar to Example 28·3, 3-cyanobenzoic acid, 3 _Methylbutyraldehyde, isocyanocyclohexane and 2-azido-phenylamine give 2_[2_(3-cyano-phenyl)-benzimidazole small group]_4_methyl-pentanoic acid ring Hexylguanamine, MS (ES+): 415 (M+H) 〇 Example 85 2-[2-(3-Gas-phenyl)-benzimidazolyl]-4-methyl-pentanoic acid cyclohexyl decylamine Similar to Example 28.3, 3-chlorobenzoic acid, 3-methylbutanal, isocyanocyclohexane and 2-azido-phenylamine yield 2-[2-(3-a-phenyl)-benzo Imidazole-diyl]-4-mercapto-pentanoic acid cyclohexyl decylamine, ms (ES + ): 415 (M+H). Example 86 N-Butyl-2-[2-(2,4-dimethoxy-phenyl)-benzimidazolyl]-2-(4-methoxy-phenyl)-acetamide and examples 28.3 Similarly, 2,4-dimethoxybenzoic acid, 4-methoxybenzoic acid, isocyanobutane and 2-azido-phenylamine give Ν-butyl-2-[2-(2 , 4-dimethoxy-phenyl)-benzimidazol-1-yl]_2-(4-methoxy-phenyl)-acetamide, MS (ES+): 474 (M+H). Example 87 N-Benzyl-2-[2-(3-decyloxy-phenyl)benzoxazole small base 4_phenyl-butanamine hydrochloride 121967.doc •102· 200811112 Similar to Examples 3.1-3.2, 3-methoxybenzoic acid, 3-phenylpropanal, isocyanoquinone and N-t-butoxycarbonylphenylenediamine gave the N-benzyl group as a brown solid. -[----methoxy-phenyl-benzimidazole-indole-yl b'-phenyl-butylamine hydrochloride, MS (ES+): 476 (M+H). Example 88 2-(4-Gas-phenyl)-2-[2-(2,3-dimethoxy-phenyl)-benzimidazol-4-yl]-N-isopropyl-acetamide Similar to Example 28.3, 2,3-dimethoxybenzoic acid, cardiochlorobenzaldehyde, iso-isocyanide and 2-azido-phenylamine produced 2-(4-gaso-phenyl)_2_[2_ ( 2,3-Dimethoxy-phenyl)-benzimidazole, benzylidene isopropylacetate, MS (ES+): 464 (M+H). Example 89 N_Butyl-2-[2-(2,4-dimethoxy-phenyl)benzimidazolyl]_2_(4-dimethylamino-phenyl)-ethenylamine analogous to Example 28.3 , 2,4-dimethoxybenzoic acid, cardiodimethylaminobenzaldehyde, isocyanobutane and 2-azido-phenylamine to produce N_butyl_2_[2_ (2,4 -dimethoxy-phenyl)-benzoxanthene small group]_2_(4-dimethylamino-phenyl)-acetamide 'MS (ES+) ·· 487 (M+H). Example 90 2-[2·(4-Phenyl-phenyl)-benzopyranoyl], isopropyl-4-phenyl-butanamine similar to Example 28.3, 4-hydroxybenzoic acid, phenylphenyl Aldehyde, isopropenyl isopropyl cyanide and 2·® nitro-phenylamine give 2_[2_(4_carbyl-phenyl)-benzoxazol-1-yl]-indole-isopropyl_4_ Phenyl-butanamine, Ms (es+): ο* 121967.doc • 103 - 200811112 (M+H). Example 91 2-[2-(4-Pyly-phenyl)-benzimidazolyl]- 4_mercapto-pentanoic acid cyclohexyldecylamine is similar to Example 28.3, 4-hydroxybenzoic acid, 3-methylpropanal, isocyanocyclohexane and 2-azido-phenylamine yielding 2-[ 2-(4-Hydroxy-phenyl)-benzimidazole small group]I methyl-pentanoic acid cyclohexyl decylamine, MS (ES+): 406 (M+H). 92 2_[2-(3_Gas-Benzyl)_Benzimido]Isopropyl phenyl phenylbutanamine is similar to Example 28.3, 3- benzoic acid, 3-phenylpropanal, isocyanide Isopropanation and 2-azido-phenylamine give 2-[2-(3-a-phenyl)-benzamidazolyl]-N-isopropyl-4-phenyl-butanamine Ms (ES+): 432 (M+H). Example 93 N-butyl-2-(4-carbo-phenyl)_2_[2 gas 2,4-dimethoxy-phenyl&gt;benzimidazole_ 1-yl]-acetamide is similar to Example 28.3, 2,4-dimethoxybenzoic acid, 4-oxobenzaldehyde, isocyanobutane and 2-azido-phenylamine to give N-butyl _ 2_(4_Chloro-phenyl)_ 2-[2-(2,4-dimethoxy-phenyl)-benzimidazol-1-yl]-acetamide, MS (ES+): 478 (M +H) 〇 Example 94 - s-cyano-phenyl-benzimidazole ^ butyl isopropyl-p-phenyl-butanamine similar to Example 28.3, 3-cyanobenzoic acid, 3_ Phenylpropanal, isopropane isopropane and 2-azido-phenylamine give 2_[2-(3-cyano-phenyl)-benzoimidine 121967.doc -104- 200811112. ]]-N-isopropyl-4-phenyl-butanamine, MS (ES+): 423 (M+H). Example 95 2-[2-(4-Ethyl-phenyl)-benzo _ azole small base · 异丙_isopropyl·2-(4-decyloxy-phenyl)ethenylamine is similar to Example 28.3, 4-ethylmercaptobenzoic acid, 4-decyloxybenzoate, isopropenyl isopropylate And 2-azido-phenylamine to give 2_[2-(4-ethylindenyl-phenyl)-benzomiso-1-yl]-indole-isopropyl-2-(4-decyloxy) -phenyl)acetamide, MS (ES + ) : 442 (Μ + Η). Example 96 [Isopropylaminocarbazyl-(4-methoxy-phenylmethylpyrazine]-benzoxazol-2-yl}-benzoic acid methyl ester is similar to Example 28·3, p-phenylene Monomethyl formate, 4-methoxybenzoic acid, isopropenyl isocyanide and 2-azido-phenylamine give 4_{ΐ_[isopropylaminemethanyl-(4-methoxy-benzene) Methyl)-methyl]-1Η-benzimidazole-2• propyl benzoate, MS (ES+): 458 (Μ+Η). Example 97 4-[1-(isopropylaminocarbazinyl-benzene) Methyl-methyl}-111-benzimidazole_2-ylbenzoic acid methyl ester is similar to Example 28.3, monomethyl terephthalate, benzaldehyde, iso-isocyanide and 2-g-nitro-phenyl The amine produced 'p-isopropyl isopropyl carbenyl-phenyl-methyl) 1H-stanoimidazole-2-yl}-benzoic acid methyl ester, Ms (es+): 428 (M+H). Example 98 121967 .doc -105- 200811112 N-Isopropylmethyl-1H-pyrrolyl)-benzimidazolyl] Phenyl-butanamine Similar to Example 28·3, 1-methyl-1H-pyrrole-2-carboxylic acid , 3·Phenylpropanal, isopropanyl isopropane and 2-azido-phenylamine are produced]^isopropyl_2_[2_(1-methyl-1H-pyrrol-2-yl)-benzo Imidazole _丨_yl]_4_phenyl-butanamine, MS (ES+) : 401 (M+H) 〇 Example 99 2-[2-(3-Cyano-phenyl)-benzimidazole-; 1-pipercapto isopropyl decylamine is similar to Example 2 8 · 3, 3 -Cyanobenzoic acid, valeric acid, isopropenyl isocyanide and 2-azido-phenylamine to give 2-[2-(3-cyano-phenyl)-benzimidazole-buki]-hexanoic acid Isopropyl decylamine, MS (ES+): 375 (M+H). Example 100 2_[2-(4-P-Phenyl-phenyl)-benzimidazole "-Isopropyl valerate" is similar to Example 28.3, 4-hydroxybenzoic acid, butyraldehyde, iso-isocyanide and 2-Azido-phenylamine yields 2-[2-(4-hydroxy-phenyl)-benzimidazolyl]-pentanoic acid isopropylamine, MS (ES+): 352 (M+H). 101 2-Benzo[1,3]dioxolyl-N-butyl_2-[2-(1_methyl-1H-°Pilo-2-yl)-benzoacene -1_ kibamine is similar to Example 28·3, 1-methyl-1H·pyrrole-2-carboxylic acid, benzo[1,3]dioxolane-5-carboxaldehyde, isocyanobutane And 2_azido-phenylamine to produce 2_benzo[1,3]dioxol-5-yl-indole-butylmethyl_m_debidoyl)-benzimidazole small group Indoleamine, MS (ES+): 431 (M+H) 〇121967.doc -106 - 200811112 Example 102 2-Cyclohexyl-2 _ [2-(2,4-dimethoxy-phenyl)-benzo Methyl succinyl (2,6-dimethyl-phenyl)-acetamide is similar to Example 28.3, 2,4-dimethoxybenzoic acid, cyclohexanecarboxylic acid, 2-isocyano-1, 3-Dimethyl-benzene and 2-azido-phenylamine give cyclohexyl-2-[2-(2,4-dimethoxy-phenyl)-benzoimine -1-yl]-(2,6-dimethyl-phenyl)-acetamide, MS (ES+): 498 (M+H). Example 103 2,N&quot;Dicyclohexyl_2-[2 -(2,4-Dimethoxyoxyphenyl)-benzimidazolyl]-Ethylamine is similar to Example 28.3, 2,4-dimethoxybenzoic acid, cyclohexanecarbaldehyde, isocyanide Alkyl and 2-azido-phenylamine diamine give 2,N-dicyclohexyl_2_[2_(2,4-dimethoxy-phenyl)benzimidazolyl]· acetamidine as a colorless solid Amine, MS (ES+): 476 (M+H). Example 104 2-cyclohex-3-enylcyclohexyl-2-[2-(2,4-dimethoxy-phenyl)-benzimidazole -1- Benzylamine is similar to Examples 2.1-2.2, 2,4-dimethoxybenzoic acid, cyclohex-3-enecarboxylic acid, isocyanocyclohexane and N-tert-butoxycarbonylbenzene The diamine produces 2-cyclohex-3-enyl-indole-cyclohexyl-2-[2-(2,4-dimethoxy-phenyl)-benzimidazole-1-yl]- as a colorless solid Acetamine, MS (ES + ) : 474 (Μ + Η). Example 105 2_[2-(4-Cyano-phenyl)-benzimidazole-;[_yl]·2,Ν-dicyclohexyl - acetamidine hydrochloride 121967.doc 107- 200811112 Similar to Example 3· 1-3.2, 4-cyanobenzoic acid, cyclohexane formaldehyde, hetero-isomerization Hexane and hydrazine-t-butoxycarbonylphenylenediamine give 2_[2-(4-cyano-phenyl)-benzoxan-1 -yl]-2, fluorenyl-dicyclohexyl as a brown solid. - acetamidine hydrochloride, MS (ES+): 441 (Μ + Η). Example 106 2-Cyclohexylcyclopentyl-2-[2-(2,4-dimethoxy-phenyl)-benzimidazolyl-yl-acetamide Similar to Example 2·1-2.2, 2 , 4-dimethoxybenzoic acid, cyclohexanecarbaldehyde, isocyanatocyclopentane and N-tert-butoxycarbonylphenylenediamine to give 2-cyclohexyl-N-cyclopentyl as a milky white solid. 2·[2-(2,4-Dimethoxy-phenyl)-benzimidazole-1-yl]-acetamide, MS (ES+): 462 (Μ+Η). Example 107 2, anthracene dicyclohexyl 2 -[2-(2,4-dimethoxy-phenyl)-5,6-difluoro-benzoimin-1-yl b-amine and examples 2· 1-2.2 similar, 2,4-dimethoxybenzoic acid, cyclohexanecarboxylic acid, isocyanocyclohexane and (2-amino-4,5-difluoro-phenyl)-carbamic acid The third vinegar produced 2, Ν-dicyclohexyl-2_[2_(2,dimethoxy-phenyl)-5,6-difluorobenzimidazol-1-yl]-acetamide as a white solid , MS (ES+): 5 12 (M+H) 〇 Example 108 2,N-Dicyclohexyl丨2_(2,4-dimethoxy-phenyl)-6-methyl-benzimidazole _ 1- Alkylamine is similar to Example 3·K3.2, 2,4-dimethoxybenzoic acid, cyclohexanecarboxylic acid, isocyanocyclohexane and (2-aminol-decyl-phenyl) )_Aminocarboxylic acid third 121967.doc 200811112 Butyl ester produces 2,N-dicyclohexyl-2-[2-(2,4-dimethoxy-phenyl)·6-methyl- as a white solid Benzimidazol-1-yl]acetamimid, MS (ES+): 490 (M+H) 〇 Example 109 2-[2-(4-Gas-phenyl)-benzimidazol-1-yl]-2 , N-Dicyclohexyl-acetamide is similar to Examples 2.1-2.2, 4-benzoic acid, cyclohexane formaldehyde, isocyanocyclohexane and N-tert-butoxy Carbonyl phenylenediamine produces 2·[2_(4-Gas-phenyl)-benzimidazol-1-yl]-2,N-dicyclohexyl·acetamide, MS (ES + ) : 450 (M+H). Example 110 2,N-Dicyclohexyl-2-(2-(4-aminesulfonyl-phenyl)-benzimidazolyl-1-ylethaneamine hydrochloride is similar to Examples 3.1-3.2, 4- Amine, fluorenylbenzoic acid, cyclohexane, formaldehyde, isocyanocyclohexane and N-tert-butoxycarbonylphenylenediamine give 2,N-cyclohexyl-2-[2·(4- Amine phenyl phenyl)-benzo oxime _ 基 卜 醯 醯 盐 , , , MS MS MS MS MS MS 2 2 2 2 2 2 2 2 2 2 2 2 2 2 2 2 2 2 2 2 2 2 2 2 2 2 2 2 2 2 2 4-Dimethoxy-phenyl)-benzimidazole-I-based (1,1,3,3-tetradecyl-butyl)-acetamide is similar to κ, 28.3, 2,4-di曱-oxybenzoic acid, cyclohexane-burning plate, 2-isocyano-2,4,4-trimethylpentane and 2-azido-phenylamine give 2-rings as yellow oil Hexyl_2·[2_(2,4·dimethoxy-phenyl)-benzimidazole-1-yl]-:^-(1,1,3,3-tetramethyl-butyl)_B Indoleamine,]^(£8+):5 06 (Μ+Η) 〇121967.doc 109- 200811112 Example 112 Cyclopentyl-(cyclopentylaminecarbamyl-methyl)]_1H_benzimidazole_ 2 base}_methyl benzoate hydrochloride is similar to the examples 3.1-3.2, monomethyl terephthalate, cyclopentane formaldehyde, Cyclopentane cyanide and N-t-butoxycarbonylphenylenediamine give cyclopentyl-(cyclopentylaminomethyl carbazyl)methyl bromide benzimimidazole 2 yl}benzoic acid as a white solid Methyl ester hydrochloride, MS (ES+): 446 (M+H). Example 113 2,N-dicyclohexyl-2-(2-quinolin-6-yl-benzimidazolyldiethylamine hydrochloride The salt is similar to Example 3· 1-3.2. Quinoline-6-carboxylic acid, cyclohexanecarboxaldehyde, isocyanocyclohexane and N-tert-butoxycarbonylphenylenediamine give 2,n-bicyclic ring as a white solid. Hexyl-2-(2-quinolin-6-yl-benzimidazole-bu)-ethyl acetate hydrochloride, MS (ES+): 467 (M+H). 2-(4-Amino-phenyl)-benzimidazole I, 2,] Dicyclohexyl-acetamide is similar to Example 2· 1-2.2, 2-ethylaminobenzoic acid, cyclohexyl Formaldehyde, isocyanatocyclohexane and N-tert-butoxycarbonylphenylenediamine produce a white solid in the process of de-ethylation of the 4-ethyl fluorenyl group. 2-(4-Amino-phenyl)-benzoimylidene-1-yl 2,N-dicyclohexyl-acetamide, MS (ES + ) : 43 1 (M+H) 〇 Example 115 2 -[2-(2,4-dimethoxy-phenyl)-benzene Imidazol-1-yl]_5-phenyl-pentanoic acid cyclohexyl decylamine hydrochloride 121967.doc -110- 200811112 115.1 tetrapropylammonium bromide (VII) (117 mg, 〇·33 mm〇1, 〇1 equivalent) Add to 4-methyl praline n-oxide (580 mg, 5.00 mmol, 15 rpm) and 4-phenylbutanol (5 〇〇 mg, 3.33 mmol, 1·〇 equivalent ) in a solution of B in (30 mL). The reaction mixture was stirred at room temperature for 6 hours then filtered through celite® and then filtered over EtOAc EtOAc (EtOAc). The solvent was evaporated and the crude was purified by flash chromatography eluting elut elut elut elut elut elut Mg (yield 13%). 115.2 Similar to Example 3· 1-3.2, 2,4-dimethoxyoxybenzoic acid, 4-phenylbutane, isocyanocyclohexane and N-tert-butoxycarbonylphenylenediamine were produced as a brown solid. 2-[2-(2,4-Dimethoxy-phenyl)-benzimidazole-stiryl-pentanoic acid cyclohexyl decylamine hydrochloride, MS (ESI): 512 (M+H). Example 116 4-[1-(1-Cyclopentylaminecarbazinyl-3-phenyl-propyl)-1 -benzimidazol-2-ylbenzoic acid methyl ester Similar to Example 2.1-2.2, oxime Benzocarbonylbenzoic acid, 3-phenylpropanal, isocyanatocyclopentane and N-t-butoxycarbonylphenylenediamine give 4-[1-(1-cyclopentylamine) as a white solid Methyl 3-(phenyl-propyl)-1 - benzo-pyridin-2-yl]-benzoate, MS (ES+): 482 (M+H). Example 117 2,N-Dicyclohexyl-2-[2-(4-dimethylaminesulfonyl-phenylbenzimidazolyl)-ethanoamine hydrochloride 121967.doc -111 - 200811112 with Example 3.1 -3.2 Similarly, 4-didecylamine sulfonylbenzoic acid, cyclohexane decanoic acid, isocyanocyclohexane and N-tert-butoxycarbonylphenylenediamine give 2,N-di. Cyclohexyl-2-[2-(4-didecylaminesulfonyl-phenyl)-benzimidazol-1-yl]acetamide hydrochloride, MS (ES+) ·· 523 (M+H) Example 118 2,N-Dicyclohexyl 2 -[2-(3-aminesulfonyl-phenyl)-benzimidazol-1-ylbutylidene hydrochloride is similar to Example 3· 1-3.2 , 3-amine sulfonyl benzoic acid, cyclohexane formaldehyde, isocyanatocyclohexane and N-tert-butoxycarbonyl phenylenediamine give 2,N- yi hexyl group as a brown oil. 2-[2-(3-Amine-flavoryl-phenyl)-benzoate. Sodium]-acetamide hydrochloride, MS (ES+) ··495 (Μ+Η). Example 119 2,N -Dicyclohexyl-2_{2·[3-(1Η_tetrazole s· kibphenylbenzimidazolylpyridinium hydrochloride is similar to Example 3.1-3.2, 3-(111-tetrazole) _5-yl)-benzoic acid, cyclohexane citric acid, isocyanide cyclohexane and Ν-t-butoxycarbonylphenylenediamine produces 2,y-dicyclohexyl-2-{2-[3-(1Η-tetrazol-5-yl)-phenyl]-benzene as a yellow oil And imidazol-1-yl acetamide hydrochloride, MS (ES+): 484 (Μ + Η). Example 120 2, Ν-dicyclohexyl-2-{2-[4-(1Η-imidazole·2 · phenyl)benzimidazole_1β benzylamine hydrochloride is similar to Example 3· 1-3.2, 4-(1Η-imidazol-2-yl)-benzoic acid, cyclohexaneformaldehyde, iso Cyanide cyanide and hydrazine-t-butoxycarbonylphenylenediamine give 2, anthracene-dicyclohexyl-2·{2-[4-(1Η-imidazol-2-yl)- Phenyl]_ 121967.doc • 112· 200811112 Benzo-salt-s-l-yl}-acetamide hydrochloride, MS (ES+): 482 (M+H). Example 121 2,N-dicyclohexyl- 2-[2-(4-Imidazolyl+yl-phenyl)-benzimidazole-I-diethylacetamide hydrochloride is similar to Example 3 · 1 - 3 · 2, 4-Miso-1 -yl-benzoic acid Cyclohexane carboxylic acid, isocyanocyclohexane and N-tert-butoxycarbonyl phenylenediamine give 2,N-dicyclohexyl-2-[2-(4-imidazol-1-yl) as a brown solid -Phenyl)·benzimidazol-yl]•Ethylamine hydrochloride, MS (ES + ) : 482 (M+H). 2,N-cyclohexyl-2-[2-(4-[l,2,4]triazin-4-yl-phenyl)benzoxanthine β&gt;l&gt;β-[]-acetamide hydrochloride Example 3.1_3.2 is similar, 4-[1,2,4]trimethyl-4-benzo-benzoic acid, cyclohexanefurfural, isocyanocyclohexane and N-tert-butoxycarbonylphenylenediamine Producing 2,N-dicyclohexyl-2_[2_(4-[1,2,4]triazol-4-yl-phenyl&gt; benzo-salt-1·yl] in the colorless oil Indole hydrochloride, MS (ES+): 483 (M+H) 〇 Example 123 2'N-cyclohexyl-indole 1!!-pyrazole-4·yl)-phenylbenzimidazole-1-yl b Indoleamine hydrochloride is similar to κ3.1·&quot;3.2, 4-(1Η-pyrazol-4-yl)-benzoic acid, cyclohexanecarboxylic acid, hetero-cyclized cyclohexane and sensed third butoxide Benzyl phenylenediamine produces 2,1 dicyclohexyl-2]2-[4-(1!1-pyrazol-4-yl)-phenyl]-benzimidazole small group B as a colorless oil Indole hydrochloride, MS (ES+): 482 (Μ+Η). Example 124 121967.doc 200811112, cyclohexyl 2 [2_(4-[1,2,3] succin-4-yl-phenyl)-benzopyrene-1-yl]-acetamide hydrochloride ', similar to the example H 3 · 2, 4-[1,2,3]thiadiazol-4-yl-benzoic acid, cyclohexanecarboxaldehyde, isocyanocyclohexane and N_t-butoxycarbonyl Phenylenediamine produces a colorless oil of 2,N-dicyclohexyl_2_[2_(4_[1,2,3]嗟>sodium 4-yl-phenyl)benzonitrile-1-1 Acetamide hydrochloride, Ms (ES+): 5〇〇(M+H) 〇Example 125 2,N-Dicyclohexyl_2_[2_(1,3_di-oxo-2,3-dinitrogen异 哚 哚 _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ 5-carboxylic acid, hexane hexane formaldehyde, isocyanocyclohexane and hydrazine-t-butoxycarbonyl phenylenediamine give 23-dicyclohexyl-sodium 4-yl-phenyl) as a yellow oil. Benzimidazole-丨-yl]-acetamide hydrochloride, (ES+): 485 (M+H) 〇 Example 126 2,N-Dicyclohexyl-2-[2_(3-tetrazolyl)phenyl Benzimidazolylacetamide hydrochloride is similar to Examples 3.1-3.2, 3-tetrazol-1-ylbenzoic acid, cyclohexane Aldehyde, isocyanocyclohexane and N-t-butoxycarbonylphenylenediamine give 2,N-dicyclohexyl-2-[2-(3-tetrazol-1-yl-) as a colorless oil Phenyl)-benzimidazole _ bromo]-acetamide hydrochloride, MS (ES+): 484 (M+H). Example 127 4-[1-(cyclohexyl-3-methoxycarbonylphenyl) Aminomethylidene-methyl)-1Η_benzo-121967.doc -114- 200811112 Methyl imidazol-2-ylbenzoate hydrochloride is similar to the examples 3.1-3.2, monomethyl terephthalate, cyclohexane Alkanal, 3-methyloxycarbonylphenyl and N-tert-butoxycarbonylphenylenediamine give 4-[1-(cyclohexyl-3-methoxycarbonylphenylamine) as a white solid Methyl hydrazino _ methyl MH- benzimidazol-2-yl]-benzoic acid methyl ester hydrochloride, MS (ES + ) : 526 (M+H). Example 128 Anti 4-(1-{cyclohexyl- [(4-Methoxycarbonyl-cyclohexyldecyl)-amine-mercaptopurine methyl 1H-benzimidazol-2-yl)-benzoic acid methyl ester hydrochloride is similar to Example 3· 1-3.2, p-benzene Monodecyl dicarboxylate, cyclohexanefurfural, methyl 4-isocyanomethylcyclohexane decanoate and N.3 butyloxycarbonylphenyldiamine give the anti-4- (1-{cyclohexyl-[ (4-Methoxycarbonyl-cyclohexyldecyl)-amine-methylmethyl]-methyl}-1Η-benzoimidazol-2-yl)-benzoic acid methyl ester hydrochloride, MS (ES+): 546 (M+H). Example 129 4-{2-cyclohexyl-2-[2-(4-methoxyphenyl-phenyl)-benzoxanthino-1-yl]-ethenylaminopiperidine-1-decanoic acid Ethyl ester hydrochloride is similar to Example 3· 1-3.2, monomethyl terephthalate, cyclohexane formaldehyde, ethyl 4-isocyano-piperidine-1-carboxylate and N-tert-butoxycarbonyl Phenylenediamine gives 4-{2-cyclohexyl-2-[2-(4-methoxycarbonyl-phenyl)-benzoimin-1 -yl]-ethenylamino} as a white solid.唆-1 - ethyl formate hydrochloride, MS (ES + ) : 547 (M+H) 〇 Example 130 N·cyclohexyl-2-[2-(2,4-dimethoxy-phenyl) -benzimidazol-1-yl]·2-benzene 121967.doc -115- 200811112 The base-acetamide hydrochloride is similar to the examples 3.1-3.2, 2,4-dimethoxy-benzoic acid, benzofural , isocyanocyclohexane and N-t-butoxycarbonylphenylenediamine give N-cyclohexyl-2-[2-(2,4-dimethoxy-phenyl)·benzone as a white solid Methyl imide-acetamide hydrochloride, MS (ES+): 470 (M+H). Example 131 4_(1_{cyclohexyl-[3_(2-o-oxy-pyrrolidine·1β-propylpropylcarbamyl)-methylphen 1H-benzimidazol-2-yl)-benzoic acid oxime hydrochloride The salt is similar to Example 3· 1-3.2, monomethyl terephthalate, cyclohexane formaldehyde, 1-(3-isocyano-propyl)-pyrrolidin-2-one and N-tert-butoxy Carbonylphenylenediamine produces 4_(1_{cyclohexyl-oxy-pyrrolidinyl)-propylamine-methylhydrazino]-methyldibenzimidazole-2-yl) in a colorless oil Methyl benzoate hydrochloride, MS (ES + ) ·· 517 (M+H). Example 132 4-U-[Cyclohexyl-(3-methoxycarbonyl-propylamine-methylmethylmethyl]·1Η-benzopyran-2-yl}-benzoic acid oxime ester hydrochloride and Example 3 · 1-3.2 similar, monomethyl terephthalate, cyclohexane formaldehyde, 4-isocyano-butyric acid methyl ester and hydrazine _ third butoxy carbonyl phenylenediamine produced as a colorless oil 4- {1-[Cyclohexyl-(4-methoxycarbonyl-propylaminecarbamimidyl)-methyl; ΜΗ_stanoimidazol-2-yl}-benzoic acid methyl ester hydrochloride, Ms (ES + ) : 492 (M+H) 〇 Example 133 4-{1[cyclohexyl-(4-methoxycarbonyl-butylamine-methyl hydrazinyl-methyl bromide-p-benzopyranyl benzoic acid methyl ester hydrochloride 121967. Doc -116- 200811112 Similar to Examples 3.1-3.2, monomethyl terephthalate, cyclohexane formaldehyde, 5-isocyano-pentanoic acid methyl ester and N-third butoxycarbonylphenylenediamine produced colorless Oil 4-{1-[cyclohexylmethoxycarbonyl-butylaminecarbazyl)-methyl]-1H-benzoimidazole-2-yl}-benzoic acid methyl ester hydrochloride, LC 215 nm; Rt 2.13 : 100%, MS (ES + ) : 506 (M+H) 〇 Example 134 4-{1-[cyclohexyl-(5-methoxycarbonyl-pentylaminecarboxylidene)- Methyl]-1H-benzoim Methyl-2-yl}-benzoic acid methyl ester hydrochloride is similar to Example 3·1 -3·2, monomethyl terephthalate, cyclohexane formaldehyde, methyl 6-isocyano-hexanoate and hydrazine -T-butoxycarbonylphenylenediamine produces 4-{1-[cyclohexyl-(5-methoxycarbonyl-pentylaminomethyl)-methyl]-1 fluorene-benzoate as a colorless oil Imidazolyl-2-yl}-benzoic acid methyl ester hydrochloride, Ms (ES + ) : 520 (M+H) 〇 Example 135 2_cyclohexyl_2_[2_(2,4-dimethoxy-phenyl) Benzimidazole + keb N-methyl-acetamide hydrochloride is similar to Example 3· 1-3.2, 2,4-dimethoxybenzoic acid, cyclohexanecarbaldehyde, isocyanide methane and N- Tributoxycarbonylphenylenediamine produces 2-cyclohexyl-2-[2-(2,4-dimethoxy-phenyl)-benzimidazolyl]-N-methyl-acetamidine as a white solid Amine hydrochloride, Ms (ES + ): 4〇8 (M+H). Example 136 2-[2-(4-Ethylamino-phenyl)benzimidazole-1-yl]_2, ]^_Dicyclohexyl_acetamide 136.1 121967.doc -117- 200811112 Similar to Example 3· 1-3.2, 4-tert-butoxycarbonylamino-benzoic acid, cyclohexaneformaldehyde, isocyanide ring Hexane, hydrazine-tertiary butoxycarbonylphenylenediamine 2-[2-(4-Amino-phenyl)·benzimidazole-^yl]- as a white solid during the partial butoxylation of the butoxymethylaminophenyl moiety 2, Ν-dicyclohexyl-acetamide hydrochloride, ms (ES+): 431 (M+H) 〇136.2 Add acetic anhydride (175 mg, 1.71 mmol, 1·〇 equivalent) to 2_[2_(4 -yl-benzino)-benzinosin-1-yl]_2,n-dicyclohexyl-acetamide hydrochloride (Example 34) (74 mg, 1.71 mmol, 1.0 eq.) and pyridine (13 mg, 1.71 mmol, 1.0 eq.) in dichloromethane (2 mL). The reaction was stirred at room temperature for 16 hours, then re-treated with pyridine (13 mg, 171 mmol, 1.0 eq.) and acetic anhydride (17 mg, 〇n mm 〇1, 〇 当量 equivalent) and stirred at room temperature 24 hours. The reaction mixture was taken up in EtOAc (2 mL) and filtered and filtered. The solid was dissolved in hot ethyl acetate (3 mL) and filtered, and the filtrate was concentrated in vacuo to afford 2-[2-(4-ethylamino)-phenyl) Salvian-1-yl]-2,N-dicyclohexylacetamide, 26 mg (32%), MS (ES+): 473 (M+H). Example 137 2-[2-(3_Ethylaminophenyl)-benzimidazole small group]_2,N-Dicyclohexyl_acetamide 137·1 Similar to Examples 3.1-3.2, 3-third Butoxycarbonylamino-benzoic acid, ring 121967.doc -118- 200811112 Hexane formaldehyde, isocyanocyclohexane, N-tert-butoxycarbonylphenylenediamine with concomitant 3-tert-butoxycarbonyl 2-[2-(3-Amino-phenyl)-benzimidazole-;[_yl]-2,N- as a white solid during the decyloxycarbonylation of the aminophenyl moiety Dicyclohexyl-acetamide hydrochloride, MS (ES+): 431 (M+H). 137.2 Similarly to Example 136.2, 2-[2-(3-Amino-phenyl)-benzimidazolyl-1-yl]-2,N-dicyclohexyl-acetamide hydrochloride afforded as a colorless oil. 2_[2_(3-Ethylamino)phenyl)-benzoimin-1-yl]-2,N-dicyclohexyl-acetamide, MS (ES + ) : 473 (M+H 〇 Example 138 [cyclohexyl-(3-decylamino-phenylamine-carbenyl)-methyl]an-benzoimidazol-2-yl}-benzoic acid methyl ester hydrochloride 138.1 and Example 3· Similar to 1-3.2, terephthalic acid monomethyl ester, cyclohexane formaldehyde, N-(3-isocyano-phenyl)-formamide and N-tert-butoxycarbonylphenylenediamine produce 4- {1-[(3-Amino-phenylaminocarbamimidyl)-cyclohexyl-methyl b 1H•benzimidazol-2-yl}-benzoic acid methyl ester hydrochloride, MS (ES+): 483 ( M+H). 138.2 A mixture of acetic anhydride (162 mg, 1.58 mm 〇i, 2.2 eq.) and formic acid (7 3 mg, 1.58 mmol, 2.2 eq.) was heated to 6 〇. It took 15 minutes. The reaction was cooled to room temperature and 4-{1-[(3-amino-phenylaminemethanyl)-cyclohexyl-methyl]_1H-benzimidazol-2-yl}-benzoic acid oxime ester was added ( A solution of 35 mg, 0.72 mmol, 1.0 eq. in hexanes (2 mL). The reaction mixture was washed with 1N EtOAc (2 mL). Concentrate the reaction mixture in vacuo to afford 4-{1-[cyclohexyl-(3-carbamido-phenylaminecarbazyl)-methyl]-1H-benzimidazol-2-yl as a yellow solid. Ethyl benzoate, 23 mg (yield 62%), MS (ES+): 5 11 (M+H). Example 139 N-cyclopentyl-2-(2-naphthalen-1-yl-benzimidazole-1-yl)-propanamide was similar to Example 2·1-2.2, naphthalene-1·carboxylic acid, acetaldehyde, and C-cyclopentane cyanide and N-t-butoxycarbonylphenylenediamine give N-cyclopentyl-2-(2-naphthalen-1-yl-benzofuran-1-yl)-propyl as a white solid Guanamine, MS (ES+): 438 (M+H). Example 140 2,N -*-cyclohexyl-2_(2-phenyl-benzoxanthene-1-yl)-ethinylamine Addition of benzoic acid (12.2 mg, 0.1 mmol, 1 eq.) to cyclohexane Alkyne (16.8 mg, 0.15 mmol, 1.5 equivalents), isocyanatocyclohexane (1 (). 9 mg, 0·1 mm〇hi equivalent) and N-t-butoxycarbonylphenylenediamine (Mg) In a solution of methanol (1 mL), the mixture was stirred at room temperature for 16 h. The solvent was evaporated and the crude intermediate was dissolved in EtOAc (1 mL). The TFA was evaporated and the product was isolated via preparative HPL C (gradient elution: water with 0.1% difluoroacetic acid / acetonitrile). MS (ES + ): 416 (M+H). Example 141 2-[1-(cyclohexyl-cyclohexylaminecarbazinyl-indenyl)_1Εμbenzimidazole_2-yl]-benzamide 121967.doc 120- 200811112 N-di-dibutoxy domain The basic amine (208.3 mg, 1 mmol, 1 eq.) was added to cyclohexanecarboxaldehyde (168.3 mg, ι·5 min 〇l, 1.5 eq.), isocyanocyclohexane (109.2 mg, 1 mmol, 1 equivalent) and a solution of monomethyl phthalate (180.2 mg, 1 mmol, 1 eq.) in methanol (2 mL). The mixture was stirred at room temperature for 16 hours. After evaporating the solvent, the crude intermediate was dissolved in EtOAc (10 mL). After evaporation, the crude product was dissolved in acetic acid and stirred at 80 ° C for 6 hours. After evaporation, the crude product was dissolved in ethyl acetate and extracted from aqueous NaHCI. After evaporating the organic layer, the obtained residue was dissolved in methanol (1 ml) and then treated with 2 N NaOH (5 ml) at room temperature for 16 hours. The resulting formic acid was isolated via preparative HpLc. 46 mg ((M mm 〇 1, i equivalent) was dissolved in DMF (1 ml). 38 mg (〇.l mmol, 1 eq.) of HATU was added and the mixture was stirred at ambient temperature for 10 min. Bu 1 saturate: ^ / / ^ ^ ^ solution. The reaction was stirred at room temperature for 16 hours. The product was isolated via preparative HpLC. MS (ES+): 460 (M+H) 〇 Example 142 2-[2-( 5-Amine "Bit_2_yl"_Benzene-salt + keb 2,n-dicyclohexyl-acetamide _ similar to Example 140, 5-amino, 唆_2_carboxylic acid, cyclohexyl Burning citric acid, decyl ocyanide and N-second butoxycarbonyl stupid diamine. Ms (ES+): 432 (M+H) 〇 Example 143 2'Ν·Dicyclohexyl·2_[2_(2 _Ethyl_5_methyl-2h-indenylbenzimidazole-1-yl]-acetamide 121967.doc -121 - 200811112 Similar to Example 140 '1-ethyl-3-methyl-specific Lo-5-carboxylic acid, cycloheximide, isocyanocyclohexane and N-tert-butoxycarbonylphenylenediamine. MS (ES+): 449 (M+H) 〇 Example 144 2,N-bicyclic Hexyl-2·[2-(5-methyl-isoxanth-4-yl)-benzoimin-1-ylpropiamine is similar to Example 140, 5-methylisoxazole-4-carboxylic acid , cyclohexane furfural, isocyanide cyclohexane and hydrazine - the first Tributoxy phenyl phenyl diamine MS (ES+): 421 (M+H). Example 145 2 Ν·Dicyclohexyl-2-[2-(1Η-pyrrol-2-yl)-benzimidazole _1_yl]-acetamide is similar to Example 140, pyrazolecarboxylic acid, cyclohexanefurfural, isocyanatocyclohexane and tert-butoxycarbonylphenylenediamine. MS (ES + ) : 405 (M +H) 〇 Example 146 2-(ΓΗ-[2,5']biphenylimidazolyl)_2,n_dicyclohexyl-acetamide Similar to Example 140, 5-benzimidazolecarboxylic acid, cyclohexanecarbaldehyde , isocyanocyclohexane and N-tert-butoxycarbonylphenylenediamine. MS (ES + ) : 456 (M+H) 〇 Example 147 2,~Dicyclohexyl-2-(2-furan-2 -Base-benzimidazol-1-yl)-acetamide similar to Example 140, 2-hydric acid, cyclohexanecarboxaldehyde, isocyanocyclohexane, and dibutyl carbonyl phenylenediamine. MS (ES + ): 406 (M+H). Example 148 121967.doc -122- 200811112 2-[6-Bromo-2-(4-carbo-phenyl)-benzimidazol-1-yl]-2,N-di Cyclohexyl-acetamide is similar to Example 140, 4-chlorobenzoic acid, cyclohexanefurfural, isocyanide cyclohexane, and (2-amino-4-bromo-phenyl)-amino decanoic acid third Butyl ester. MS (ES + ): 530 (M+H). Example 149 2·[6-Gas-2-(4-Gas-phenyl)·benzoxan-1-yl]-2,N-dicyclohexyl-ethenylamine similar to Example 140, 4-chlorobenzene Citrate, cyclohexanefurfural, isocyanide cyclohexane and (2-amino-4-chloro-phenyl)-carbamic acid tert-butyl ester. MS (ES + ): 485 (M+H). Example 150 2-[2-(4·Gas-phenyl)-6-methoxy-benzoxanthene-1-yl]-2,N-dicyclohexyl_acetamide is similar to Example 140, 4- Chlorobenzoic acid, cyclohexane formaldehyde, isocyanocyclohexane and (2-amino-4-methoxy-phenyl)-carbamic acid tert-butyl ester. MS (ES + ) : 481 (M+H) 〇 Example 151 2-[6-Gas-2-(4_Gas_phenyl)-5-Gas-benzoindole-1-yl]-2,N -Dicyclohexyl_acetamide is similar to Example 140, 4-chlorobenzoic acid, cyclohexane formaldehyde, isocyanocyclohexane and (2-amino-4-chloro-5-a-phenyl)- The third carboxylic acid formic acid is intended. MS (ES + ) ·· 503 (M+H). Example 152 (S)-2,N-Dicyclohexyl·2-[2-(2,4-dimethoxyphenyl)benzoindole-1_yl]-acetamide 121967.doc -123 - 200811112 Similar to Example 140, 2,4-dimethoxybenzoic acid, cyclohexanefurfural, isocyanatocyclohexane and N-t-butoxycarbonylphenylenediamine. MS (ES+): 476 (M+H) 〇 Example 153 (S)-2-[2-(4-Gas-phenyl)-benzimidazolyl]-2,N-dicyclohexyl-acetamide Example 140 is similar to 4-benzoic acid, cyclohexane formaldehyde, isocyanocyclohexane, and N-t-butoxycarbonylphenylenediamine. MS (ES+): 451 (M+H) 〇 Example 154 2-[1-(cyclohexyl-cyclohexylaminemethanyl-methylbenzimidazole_2-yl]-N-methyl-benzoguanamine Similar to Example 141, monomethyl phthalate, cyclohexane formaldehyde, isocyanocyclohexane, N-tert-butoxycarbonylphenylenediamine, and methylamine. MS (ES + ) ·· 473 ( M+H) 〇 Example 155 2,N-Dicyclohexyl_2·(2-furan-3-yl-benzimidazol-1-yl)-acetamide Similar to Example 140, 3-decanoic acid, cyclohexane Alkanealdehyde, isocyanocyclohexane and hydrazine-t-butoxycarbonylphenylenediamine. MS (ES+): 406 (Μ+Η). Example 156 2,N-dicyclohexyl-2-[2-( 3-Mercapto-furan-2-yl)-benzimidazol-1-ylpyridylamine is similar to Example 140, 3-methyl-nonanoic acid, cyclohexanecarbaldehyde, isocyanide cyclohexane, and N- Third butoxycarbonylphenylenediamine MS (ES + ) : 420 (M+H). 121967.doc -124- 200811112 Example 157 2,N-Dicyclohexyl-2-[2-(3-methyl -isoxazol-5-yl)-benzimidazolyl-1-yl]-acetamide is similar to Example 140, 3-methyl-isoxazole-5-carboxylic acid, cyclohexanecarbaldehyde, isocyanide cyclohexane Alkane and N-tert-butoxycarbonylphenylenediamine. MS (ES + ): 421 (M+ H) 〇 Example 158 2,N-Dicyclohexyl-2-(2-m-tolyl-benzimidazol-1-yl)-acetamide Similar to Example 140, m-toluic acid, cyclohexanecarbaldehyde, isocyanide Cyclohexane and N_t-butoxycarbonylphenylenediamine. MS (ES+): 430 (M+H) 〇 Example 159 2,N-Dicyclohexyl-2-[2-(3-fluoro-benzene) Benzo-benzimidazol-1-yl]-acetamide is similar to Example 140, 3-fluorobenzoic acid, cyclohexanecarbaldehyde, isocyanocyclohexane, and N-t-butoxycarbonylphenylenediamine. MS (ES + ) : 434 (M+H). Example 160 2,N-dicyclohexyl-2- [2-(2- gas-phenyl)-benzofuran-1-yl] ethylamine Similar to Example 140, 2-fluorobenzoic acid, cyclohexanecarboxaldehyde, isocyanocyclohexane, and N-t-butoxycarbonylphenylenediamine. MS (ES+): 434 (M+H). 2,N-Dicyclohexyl-2_[2-(3,5-dimethyl-isoxazol-4-yl)-benzimidazol-1-yl]-acetamide 121967.doc -125- 200811112 Example 140 is similar to aldehyde, isocyanatocyclohexane (ES+): 435 (M+H) 〇 Example 162

'3,5-Dimethylisoxazole-4-carboxylic acid, cyclohexane formazan and N-t-butoxycarbonylphenylenediamine. MS 2,N-dicyclohexyl_2_[2 decylamine (3-methyl-indol-2-yl)-benzopyrimidin-1-yl b-benzyl 140 is similar, 3_methyl_2_ Thiophenecarboxylic acid, cyclohexanecarboxaldehyde, isocyanocyclohexane and N_t-butoxy phenylenediamine. MS (ES+): 436 (m+h) 〇 Example 163 2, Ν-cyclohexyl 2-[2-(4-vinylphenyl)benzimidazolylpyridinamide is similar to Example 140, 4 -ethenylbenzoic acid, cyclohexaneformaldehyde, isocyanation of hexanone and hydrazine-tert-butoxycarbonylphenylenediamine. Ms (ES+) ·· 442 (M+H) 〇Example 164 2,N-Dicyclohexyl·2·[2-(2,3-dimethylphenyl)-benzimidazole·!·基卜The acetamide is similar to Example 140, 2,3-dimethylbenzoic acid, cyclohexanefurfural, isocyanatocyclohexane, and hydrazine-t-butoxycarbonylphenylenediamine. MS (ES+): 444 (M+H) 〇 Example 165 2,N-Dicyclohexyl-2-[2-(3,4-dimethyl-phenyl)-benzopyrimidinyl Example 140 is similar to 3,4-dimethylbenzoic acid, cyclohexanecarbaldehyde, isocyanide 121967.doc-126-200811112 hexane and 1 third butoxycarbonylphenylenediamine. MS (ES + ) ·· 444 (M+H) 〇 Example 166 'N-cyclohexyl-2-[2-(4-ethyl-phenyl)-benzimidazole β1_ylbudecamide with Example 140 Similarly, ethyl ethyl benzoic acid, cyclohexanic acid, hetero-enzymes, and hydrazine-t-butoxycarbonyl phenylenediamine. Ms (ES+) : 444 (M+H). Example 167 2,N-Dicyclohexyl-2-[2-(2,4-dimethyl-phenyl)-benzimidazolyl]B «HSttL ^3s Similar to Example 140, 2,4-dimethyl Benzoic acid, cyclohexane formaldehyde, isocyanocyclohexane and N-tert-butoxycarbonylphenylenediamine. Ms (ES+) ·· 444 (M+H) 〇Example 168 2,N-Dicyclohexyl-2-[2-(2-ethyl-phenyl)·benzimidazole-; 1-ylbudecamide Similar to Example 140, 2-ethylbenzoic acid, cyclohexanecarbaldehyde, isocyanatocyclohexane, and N-tert-butoxycarbonylphenylenediamine. MS (ES+): 444 (M+H). Example 169 2,N-Dicyclohexyl-2-[2-(4-fluoro-3-methyl-phenyl)·benzimidazole-1·ibethylamine Similar to Example 140, 4-fluoro-3 -methylbenzoic acid, cyclohexane formaldehyde, isocyanatocyclohexane and N-tert-butoxycarbonylphenylenediamine. MS (ES+) ·· 448 (M+H). 121967.doc -127- 200811112 Example 170 2'Ν·-cyclohexyl-2-[2-(3-fluoro-4-methyl-phenyl)-benzomisoyl]·acetamide is similar to Example 140 , 3-fluoro-4-methylbenzoic acid 'cyclohexanic acid, hetero-gas cyclized and hydrazine-tert-butoxy phenyldiamine. Ms (ES+) ·· 448 (M+H). Example 171 2'N--cyclohexyl (2,6.difluoro-phenyl)-benzoxanthene]]^^^^ylamine is similar to Example 14 0 '2,6-difluorobenzoic acid, cyclohexyl Burned formic acid, isocyanated % calcined and N-second butoxy phenyldiamine. MS (ES + ) ·· 452 (M+H). Example 172 2,N-Dicyclohexyl·2_[2_(3,5·difluoro-phenyl)-benzimidazole "· kibamine is similar to Example 140, 3,5-difluorobenzoic acid, ring Hexane furfural, isocyanatocyclohexane and hydrazine-t-butoxy- propyl phenyl diamine. MS (ES+): 452 (M+H) 〇 Example 173 2,N-dicyclohexyl-2-[ 2_(2,5-Difluoro-phenyl)·benzophenanthyl]-Ethylamine is similar to Example 140, 2,5-difluorobenzoic acid, cyclohexanecarbaldehyde, isocyanocyclohexane and N - tert-butoxymethyl stupid diamine. MS (ES + ) ·· 452 (M+H) 〇 Example 174 2,N-Dicyclohexyl-2_[2_(3,4-difluoro-phenyl) _ Benzimidazole small oxime is similar to Example 140 '3,4-difluorobenzoic acid, cyclohexane formaldehyde, isocyanide 121967.doc -128- 200811112 cyclohexane and N- (M+H 〇 Example 175 Butoxyl-stigromethylenediamine. MS (ES+): 452 2'N-Cyclohexyl-2_[2-(2,3-difluoro, stupyl-benzopyranyl b-amine) and examples 14 0 Similar, 2 3 - -惫!田μ ^ , Rat Benzoic Acid, Cyclohexane Formaldehyde, Isocyanide ¥ 烧 Ν Ν 第二 第二 第二 第二 第二 第二 第二 第二 第二 第二 第二 第二 ~ ~ ~ ~ ~ ~ ~ ~ ~ ~ ~ ~ ~ ~ ~ ~ ~ ~ ~ ~ ES+) : 452 (M+H) 〇Example 176 2 , N-dicyclohexyl-2, 哚{yl}_benzoxazole small group] acetamamine is similar to Example 140&quot; 弓卜朵_4-carboxylic acid, cyclohexane burning formic acid, hetero-gas cyclized cyclohexane And N-second butoxycarbonyl stupid diamine. ms (es+) : 455 (M+H) 〇 Example 177 2,N-dicyclohexyl_2_[2_(111_,_6_yl)_benzopyrene Ethylamine is similar to Example 140 &quot; 引口--6-carboxylic acid, cycloheximide, iso-cyclohexane and N-tert-butoxycarbonylphenylenediamine. MS (ES+): 々 Μ (M+H) 〇 Example 178 2-[2_(5-Athiophen-2-yl)-benzimidazolyl]_2,...dicyclohexylacetamide is similar to Example 140, 5-chlorothiophene·2_ Citrate, cyclohexanecarboxaldehyde, isocyanocyclohexane and hydrazine-t-butoxycarbonylphenylenediamine. MS (ES+): 457 (M+H) 〇Example 179 2-[2·(4-B Mercapto-phenyl)-benzimidazol-1-yl]-2,N-dicyclohexyl-ethyl 121967.doc -129- 200811112 The indoleamine is similar to the example 140, 4-ethylidenebenzoic acid, cyclohexane Furfural, isocyanatocyclohexanyl and N-second butoxycarbonyl stupid diamine. (ES+) : 458 (M+H) 〇Example 180 2-[2·(2-Ethyl-phenylbenzene And imidazolium dicyclohexyl-acetamide and examples 140 is similar, 2_acetamidobenzoic acid, cyclohexanefurfural, decyl isocyanide and N-second butoxycarbonyl stupid diamine. Ms (es+) : 458 (M+H). Example 181 2, N-cyclohexyl-2-[2-(4-isopropyl-phenyl)-benzimidazole β1-yl-bethylamine similar to Example 140, 4-isopropylbenzoic acid, cyclohexane Alkanealdehyde, isocyanocyclohexane and hydrazine-t-butoxycarbonylphenylenediamine. Ms (es+) : 458 (M+H) 〇 Example 182 2] 2_(4_Cyano-2-oxo-phenyl)_benzimidazole small group]_2,N_Dicyclohexyl-B•SBBL JJS\ Similar to Shell 140, 4-cyano-2-fluorobenzoic acid, cyclohexanecarbaldehyde, isocyanated % hexane, and N-tert-butoxycarbonylphenylenediamine. Ms (Es+) : 459 (M+H) 〇Example 183 2,N-Dicyclohexyl_2_[2_(2·Dimethylamino-phenyl)_Benzyl succinyl] acetamide Example 14 〇 Similar, 2 · - Review its dirty: its poor field is divided into 2 - T-based amine basic formic acid, cyclohexane formaldehyde, 121967.doc 200811112 oxycarbonyl phenylenediamine MS (ES+) methylamino-phenyl _benzimidazolyl isocyanatocyclohexane and N-459 (M+H) 〇 Example 184 2,N-Dicyclohexyl_2_[2_(3_diacetamide is similar to Example 140, Cyclohexane cyanide and hydrazine-459 (Μ+Η). Example 185 &quot; monomethylaminobenzoic acid, cyclohexane formaldehyde, second butoxycarbonylphenylenediamine. MS (ES+): 2,N -dicyclohexyl o-(4. methoxy_3_methyl-phenylbenzimidazole·h bis-acetamide

Similar to Example 140, 4-methoxy-3-methylbenzoic acid, cyclohexaneformaldehyde, isocyanatocyclohexane, and N_t-butoxycarbonylphenylenediamine. MS (ES + ): 460 (M+H). Example 186 2, Ν·Dicyclohexyl-2-[2-(4-methoxy-2-methyl-phenyl)benzimidazolyl]-acetamide Similar to Example 140, 4-methoxy _ 2-methylbenzoic acid, cyclohexanecarboxaldehyde, isocyanocyclohexane and N-tert-butoxycarbonylphenylenediamine. MS (ES + ): 460 (M+H). Example 187 2,N- Dicyclohexyl-2-[2-(3-methoxy-4-yl-phenyl)-benzimidazole-yl-yl]-acetamide is similar to Example 140, 3-methoxy_4_ Methylbenzoic acid, cyclohexane A 121967.doc -131 - 200811112

Aldehydes, isocyanatocyclohexane and N-tert-butoxycarbonylphenylenediamine. MS (ES+): 460 (M+H). Example 188 2,N-Dicyclohexyl-2-[2·(2-ethoxy-phenylbenzimidazol-1-yl)·acetamide Similar to Example 140, 2-ethoxybenzoic acid, ring Hexane formaldehyde, isocyanocyclohexane and hydrazine-tert-butoxycarbonylphenylenediamine. MS (ES + ): 460 (M+H). Example 189 2-[2_(6-Gas-Clidine) 3·yl)-benzimidazol-1-yl]_2,N-dicyclohexyl·acetamide Similar to Example 140, 6-chloronicotinic acid, cyclohexanefurfural, isocyanide cyclohexane and N - tert-butoxycarbonylphenylenediamine. MS (ES+): 452 (M+H) 〇 Example 190 2-[2-(2-Gas-Acridine I-based Benzimidazole-1_Kib 2, Team Dicyclohexyl-acetamide is similar to Example 140, 2_isoisonicotinic acid, cyclohexanefurfural, isocyanocyclohexane and N•t-butoxycarbonylphenylenediamine. MS (ES+) ·· 452 (M+H). Example 191 2_[2·(4-Gasylphenyl)_6-fluoro-benzimidazolyl]·2,N•Dicyclohexyl-acetamide is similar to Example 140, 4-chloro Benzoic acid, cyclohexane furfural, isocyanocyclohexane and (2-amino-4-fluoro-phenyl)-aminocarboxylic acid tert-butyl ester. ms (ES+): 468 (M+H). Example 192 2,N-Dicyclohexyl_2_[2-(3-fluoromethoxy-phenylbenzimidazole) Zolazole-Kibu 121967.doc -132- 200811112 Ethylamine f example 140 is similar, 3_gas_4_methoxybenzoic acid, cyclohexane formaldehyde, ocyanate hexane and N-third butoxide Benzyl phenylenediamine. MS (ES+): 420 (M+H) 〇 Example 193 [2 (4-gas-3-methyl-phenyl) benzimidazole- </ RTI> </ RTI> </ RTI> 2, N-dicyclohexyl -acetamide" κ, 140 similar, 4_gas_3_mercaptobenzoic acid, cyclohexanecarboxaldehyde, isocyanocyclohexane and N_t-butoxycarbonylphenylenediamine. ms (es+): 464 (M+H) 〇Example 194 [2 (3 gas-2-methyl-unyl)_benzoxanthene ^•yl]_2,^_dicyclohexylacetamide is similar to Example 140 only 3- Gas 2 - methylbenzoic acid, cyclohexane formaldehyde, isocyanocyclohexane and N 2 -butoxycarbonyl stupid diamine. ms (ES+) : 464 (M+H) 〇Example 195 2 [2 (4-Gas_3-Fluoro-p-styl)-benzimidazole-1-yl]_2,~Dicyclohexyl-acetamidamine is similar to Example 140, 4-chloro i-benzoic acid, cyclohexane-burned formic acid, Cyclohexane and N-tert-butoxycarbonylphenylenediamine.ms (ES+): 468 (M+H) 〇Example 196 2_[2_(3_Gas_4-Fluoro-phenyl)-Benzene Imidazole small group]_2,N-dicyclohexyl-acetamide and examples 140 is similar to '3-air ice fluoroformic acid, cyclohexane formaldehyde, isocyanide 121967.doc • 133- 200811112 cyclohexane and ι third butoxy (M+H) 实例 Example 197 carbonyl phenylenediamine. MS (ES + ) : 468 Μ · Dicyclohexyl _ (5-methyl·ih_ yl)-Ethylamine and Example 140 Classes of cm ^ U ' 5-methyl 吲哚_2_ decanoic acid, cyclohexyl Alkanealdehyde, isocyanocyclohexane and N-fluorene-Diso-dibutoxycarbonylphenylenediamine. MS (ES + ) : 469 (M+H) 〇 Example 198 2,N-Dicyclohexyl_2_[ M2 3 4-nonylamine two shells 140 are similar to '2,3,4·trifluorobenzoic acid, cyclohexanecarbaldehyde, isocyanine and ^t-butoxycarbonylphenylenediamine. MS (ES + ) : 470 (M+H) 〇 Example 199 吲哚-2-yl)-benzimidazole-1-fluoro-phenyl)-benzimidazol-1-yl]•B 2,N' decyl hexyl-2- [2_(2,4,5-trifluoro-phenyl)-benzimidazole_1·yl]-B" is only 140 similar to '2,4,5-trifluorobenzoic acid, cyclohexane formaldehyde, different Cyclohexyl cyanide and N-tert-butoxy (M+H) 〇 Example 200 carbonyl phenylenediamine. MS (ES + ) : 47〇2-(2_ 笨和[b]thiophene-2_yl_ Benzo-amidozol-1-yl)-2,N-dicyclohexyl-ethyl" 140 is similar to 'stupid thiophene-2-carboxylic acid, cyclohexane formaldehyde, isocyanide 121967.doc -134- 200811112 % calcined and N-second butoxy phenylenediamine. (10) (es + ) : (M+H). Example 201 2,N-Dicyclohexyl_M2_(5_Fluoro-1 Η 〇 丨嗓 丨嗓 _ _ _ _ 】 】 】 】 】 】 】 与 与 与 与 与 与 与 与 与 与 与 与 与 与 与 与 与 与, cyclohexane formaldehyde, isocyanide cyclohexane and hydrazine-second butoxycarbonyl phenylenediamine. Ms (es+) : (M+H). Example 202 Benzopyrene + Benzyl benzofuran) _2, Nc cyclohexyl-acetamide Similar to Shell 140, benzothiazole 2 -carboxylic acid, cyclohexane formaldehyde, isocyanide cyclohexane And N-t-butoxycarbonylphenylenediamine. Ms (ES+): 473 (M+H). Example 203 2,N-Dicyclohexyl_2_[2_(4-isopropoxy-phenyl)-benzimidazole^-yl]-acetamide is similar to Example 140, 'isopropoxybenzoic acid, ring Hexane formaldehyde, hetero-enriched, and N-tert-butoxycarbonylphenylenediamine. Ms (ES+): 475 (M+H) 〇Example 204 2,N•Dicyclohexyl_2_[2_(3,4-dimethoxy-phenyl)-benzimidazole-Iyl]-acetamide Similar to Example 140, 3,4-dimethoxyoxybenzoic acid, cyclohexanecarbaldehyde, heterogeneous % calcined, and third butoxycarbonylphenylenediamine. Ms (ES+): 476 121967.doc -135- 200811112 (M+H). Example 205 2,N-Dicyclohexyl-2·[2-(2,5-dimethoxy-phenyl)-benzimidazol-1-yl]-acetamide Similar to Example 140, 2,5_ Dimethoxybenzoic acid, cyclohexane formaldehyde, cyclohexyl isocyanide and N-tert-butoxycarbonylphenylenediamine. MS (ES+) ·· 476 (M+H). Example 206 2,N-Dicyclohexyl-2_[2_(2-difluoromethoxy-phenyl)-benzimidazole "· base] _ acetamide is similar to Example 140, 2-(difluoromethoxy) Benzoic acid, cyclohexanecarboxaldehyde, iso-nitriding cyclohexane and N-tert-butoxycarbonylphenylenediamine. ms (ES+): 482 (M+H). Example 207 2,N-dicyclohexyl- 2-[2_('Difluoromethoxy-phenyl-benzimidazolyl]·acetamide is similar to Example 140, 4-(difluoromethoxy)benzoic acid, cyclohexane, and isocyanide Cyclohexane and N-tert-butoxycarbonylphenylenediamine MS (ES+): 482 (M+H). Example 208 2,N-dicyclohexyl-2_[2_(3_difluoromethoxybenzene) Base) - acetamide is similar to Example 140, 3-(difluoromethoxy)benzoic acid, cyclohexane formaldehyde, isocyanocyclohexane and N-tert-butoxycarbonyl Phenylenediamine. Ms (es+): 121967.doc ... 200811112 482 (M+H) 〇Example 209 2,Ν-Dicyclohexyl-2-[2-(4-trifluoromethyl-phenyl)-benzo Imidazolyl-l-ylbenzamide is similar to Example 140, 4-trifluoromethylbenzoic acid, cyclohexanecarbaldehyde, isocyanatocyclohexane and N-t-butoxycarbonylphenylenediamine. MS (ES + ) : 484 (M+H 〇 Example 210 2,N-Dicyclohexyl-2-[2-(3,4-di-phenyl)-benzimidazol-1-yl]-acetamide is similar to Example 140, 3,4- Dibenzoic acid, cyclohexane formaldehyde, isocyanocyclohexane and N-tert-butoxycarbonylphenylenediamine. MS (ES+): 485 (M+H) 〇 Example 211 2-[2_(4_ -Phenyl)-benzoxazole small base 2,~dicyclohexyl_acetamide is similar to Example 140, 4-bromobenzoic acid, cyclohexanefurfural, isocyanatocyclohexane and N· Tributoxycarbonylphenylenediamine MS (ES+) ··495 (M+H). Example 212 2,N-Dicyclohexyl-2_[2_(6-decyloxy-naphthalene-2-yl)·benzene And imidazolium-1_yl]-acetamide is similar to Example 140, 6-methoxy-2-naphthoic acid, cyclohexane formaldehyde 'isocyanocyclohexane and N-tert-butoxycarbonylphenylenediamine MS (ES+): 497 (M+H) 〇Example 213 121967.doc -137- 200811112 2'Ν·Dicyclohexyl_2_[2♦Trifluoromethoxyphenyl)_stupid and salivary · Acetamide is similar to Example 140, 3 · (trifluoromethoxy) benzoic acid, cyclohexane formaldehyde, isocyanide cyclohexane and hydrazine - tert-butoxycarbonyl phenylenediamine. Ms (es + wide 500 (M+H) 〇Example 214 2,N-Dicyclohexyl Base 2_[2-(7-ethoxy-benzo-buttering·2_yl)-benzoxazole small group]-acetamide is similar to Example 140, 7-ethoxybenzofurancarboxylic acid, ring Hexane formaldehyde, isocyanocyclohexane and N-tert-butoxycarbonylphenylenediamine. MS (ES + ): 500 (M+H). Example 215 2,N-Dicyclohexyl-2-[2-(3-fluoro-4-trifluoromethyl-phenyl)-benzimidazole a·yl]-acetamide Similar to Example 140, 3·Fluorine 4-(Trifluoromethyl)benzoic acid, cyclohexanecarboxylic acid, isocyanocyclohexane and N-tert-butoxycarbonylphenylenediamine. MS (ES + ) : 502 (M+H) 〇 Example 216 2,~Dicyclohexyl-2-[2_(6-diethylamino--. _3_ base) 11_Benzene- 1-yl]-acetamide will be 90 mg 2-[2-(6-gas-° ratio -3-yl)-benzoimin-1-yl]_2,&gt;^-dicyclohexyl-B Indoleamine (Example 1 89) (0.2 mmol, 1 eq.) was dissolved in dmF (1)

In ml). 102 μl (1 mmol, 5 equivalents) of diethylamine was added. The mixture was heated to 120 ° C for 15 minutes using microwave heating. The product was isolated via preparative HPLC 121967.doc • 138-200811112. MS (ES + ): 489 (M+H). Example 217 2-[2-(2-Gas-5-methyl-phenyl)-benzimidazole β1-yl b 2,N-dicyclohexyl-acetamide is similar to Example 140, 2-chloro-5- Methyl benzoic acid, cyclohexane formaldehyde, isocyanocyclohexane and N-tert-butoxycarbonyl phenylenediamine. Ms (ES+): 464 (M+H) 〇 Example 218 gas-2-methyl·phenyl)_benzimidazole_1βyl 2,n-dicyclohexyl-acetamide similar to Example 140, 5- Chloro-2-methylbenzoic acid, cyclohexane formaldehyde, isocyanocyclohexane and N-tert-butoxycarbonylphenylenediamine. MS (ES+) ·· 464 (M+H). Example 219 2_[2_(2-Ga-6-methyl-phenyl)-benzimidazolyl-1-yl]·2, fluorenyl-dicyclohexyl·acetamidine similar to Example 140, 2- gas-6- Methyl benzoic acid, cyclohexane formaldehyde, isocyanide cyclohexane and hydrazine-tert-butoxycarbonyl phenylenediamine. MS (ES+): 464 (M+H) 〇 Example 220 2,N-dicyclohexyl-2-(2-quinolino-6-yl-benzimidazol-1-yl)-acetamide and Example 140 Similarly, quinololine-6-decanoic acid, cyclohexane formaldehyde, isocyanatocyclohexane, and N-t-butoxycarbonylphenylenediamine. MS (ES+): 468 (M+H) 〇 121967.doc -139- 200811112 Example 221 Ν-Dicyclohexyl-acetamide A carbaryl, isocyanide. MS (ES+): 468 2-[2-(5-Gas-2-fluoro-phenyl)-benzoxanthene-1-dibu 2 Similar to Example 140, 5-chloro-2-fluorobenzoic acid, Cyclohexane and hydrazine-tert-butoxycarbonyl stupid diamine (M+H) 〇 Example 222 Dicyclohexyl·2·[2·(4·methoxy_3,5-dimethylphenyl) Benzo-indole-1-yl]-acetamide is similar to Example 140, 3,5-dimethyl-p------------------------------------------------ -Third butoxides_立〇 ^

Milky carbonyl phenylenediamine. MS (ES+): 475 (M+H). Example 223 2,N-Dicyclohexyl 2 oxa (2,3-dimethoxy-phenyl)-benzoindole small oxime is similar to Example 140, 2,3-dimethoxybenzoic acid , cyclohexane formaldehyde, isocyanatocyclohexane and N_t-butoxycarbonylphenylenediamine. MS (ES+): 476 (M+H). Example 224 2-[2-(3-Gas_4-methoxy-phenyl)-benzimidazole Dicyclohexyl_Ethylamine is similar to Example 140, 3-chloro-4-methoxybenzoic acid, ring Hexane formaldehyde, iso cyanide cyclohexane and hydrazine-tert-butoxycarbonyl phenylenediamine. Ms (ES+): 481 (M+H). Example 225 121967.doc -140· 200811112 2,N-Dicyclohexyl 2 oxime, 5 · one gas · Benzo broad benzimidazol-1-yl]-acetamide is similar to Example 140 ^ _ ρ ^ \Τ , , 5_ di-benzoic acid, cyclohexane formaldehyde, isocyanated % hexanthene and oxime -: ^ butyloxycarbonyl phenylenediamine. MS (ES+) ·· 485 (M+H). Example 226 2-[2-(3-Gas-2,4-digas-rolling base)-benzimidazol-1-yl]-2,N-dicyclohexyl-acetamide is similar to Example 140. ^ • 虱_2,4·difluorobenzoic acid, cyclohexanecarbaldehyde, hetero-gas cyclized and fluorene-butyl-amp; butyl butyl carbonyl phenylenediamine. MS (ES+) ·· 486 (M+H) 〇Example 227 2-[2-(2 gas-4,5-difluoro-laughing, poor forest both base)_stupid imidazole_1-kib 2 , Ν · dicyclohexyl _ acetamidine is similar to the example 140, 2_ gas _4 a # 虱 4, 5_ - mouse formic acid, cyclohexane formaldehyde, isocyanide ring hexanthene and hydrazine - third butyl negative Voucher # j milk base rebel basic diamine. MS (ES+): 486 (M+H) 〇 Example 228 2,N-Dicyclohexyl-2-[2_(4-diethylaminophenyl) benzoin and succinyl] Ethylamine and examples Similar to 140, 4_diethylpyrene A poor field said that the sulphonic amine is basically tannic acid, cyclohexane formaldehyde, isocyanide cyclohexane and N_ third butanoxyxene. Ms (ES + ): 487 (M+H). Example 229 2 (4-Benzyl phenyl) phenyl, benzophenanyl] 2, n•dicyclohexyl-ethyl 121967.doc 141 - 200811112 The indoleamine is similar to the example 140, 4-benzylidene Benzoic acid, cyclohexane decanoic acid, isocyanocyclohexane and N. tributoxycarbonyl phenylenediamine. Ms (ES+) : 520 (M+H). Example 230 (S)-2-[2_(4_Mercapto-phenylbenzimidazolyl 2,N-dicyclohexyl·acetamide) similar to Example 140, 4-cyanobenzoic acid, cyclohexanecarbaldehyde, Isocyanation % hexanyl and N-tert-butoxycarbonyl phenylenediamine. ms (Es + ) : 441 (M+H) 〇 Example 231 2, N_: cyclohexyl_2_[2 phenoxyphenyl ) Benzene oxime small group] _ acetamamine /, κ Example 140 is similar to 'phenoxybenzoic acid, cyclohexane formaldehyde, isocyanac ring and N-tert-butoxycarbonyl phenylenediamine. MS (ES + ): 509 (M+H). Example 232, cyclohexylphenoxy-phenyl)-benzimidazolyldiethylamine II Example 140 is similar, 2-phenoxybenzoic acid, cyclohexane formaldehyde, isocyanine and the third Oxycarbonyl phenylenediamine. MS (ES+) ·· 509 (M+H) 〇 Example 233 2'N-cyclohexyl_2_[2_(3-phenoxy-phenyl-benzimidazole 4-yl)-acetamide is similar to Example 140 3_This milk is basically formic acid, cyclohexane formaldehyde, isopropylidene hexyl hexane and _dibutyloxycarbonyl phenylenediamine. MS (ES+) ·· 509 121967.doc -142- 200811112 (M+H) 〇 Example 234 2,Ν_Dicyclohexyl-2·{2-[2_(1,1,2,2-tetrafluoro-ethoxy)-phenyl]-benzoimin-1-yl}-acetamidine The amine is similar to Example 140, 2-(1,1,2,2-tetrafluoroethoxy)benzoic acid, cycloheximide, isocyanocyclohexane, and hydrazine-t-butoxycarbonylphenyldiamine. Ms (ES+): 532 (M+H). Example 235 2,]&gt;^-Dicyclohexyl-2-{2-[3-(1,1,2,2-tetraoxy-ethoxy) _Phenylbenzoxazole-l-yl}•acetamide is similar to Example 140, 3-(1,1,2,2-tetrafluoroethoxy)benzoic acid, cyclohexanecarbaldehyde, isocyanide Cyclohexane and N-tert-butoxycarbonylphenylenediamine. Ms (ES + ) : 532 (M+H). Example 236 2,N-dicyclohexyl_2-{2_[4_(1,1, 2,2_Tetrafluoro 4_ethoxy)-phenyl benzoxazole-l-yl}-acetamide is similar to Example 140, 4-(1,1,2,2-tetra Ethoxy)benzoic acid, cyclohexanecarboxaldehyde, isocyanocyclohexane and N-tert-butoxycarbonylphenylenediamine. Ms (ES+): 532 (M+H). Example 237 2, N_2 Cyclohexyl 2-[2-(4,-trifluoromethyl-biphenyl)-benzofurfuryl]-acetamide is similar to Example 140, 4f-trifluoromethyl-biphenyl-4-carboxylic acid Cyclohexane, isocyanocyclohexane and N-tert-butoxycarbonyl stupid diamine. Ms 121967.doc -143- 200811112 (ES+) : 561 (M+H) 〇Example 238 2,N- Dicyclohexyl-2-[2-(3',4'-dimethyl**4_yl)benzimidazolylamine, cyclohexanemethylamine 0 is similar to Example 140, 4-(3, 4-Dichlorophenyl)benzoic acid, isocyanatocyclohexyl and N-t-butoxymimebenzene (ES + ) : 561 (M+H) 〇 Example 239 2,N-Dicyclohexyl- 2-[2-(2,4-dioxa-5-amine sulfonyl-phenyl)-benzimidazole-1-phenylpyramine is similar to Shell 140, 2,4- oxamethazine Benzoic acid, cyclohexyl, formaldehyde, isocyanocyclohexane and N-tert-butoxycarbonylphenylenediamine. ms (ES + ) : 563 (M+H) 〇 Example 240 (S)-2_[6_ Gas-2-(4_gas-phenyl)-5-fluoro·benzo benzoate 嗤_1_ kib 2,n_bicyclic Hexyl-acetamide is similar to Example 140, 4-chlorobenzoic acid, cyclohexanecarboxaldehyde, isocyanocyclohexane and (2-amino-4-chloro-5-fluoro-phenyl)-aminocarboxylic acid Tributyl ester. Ms (ES + ) : 503 (M+H). Example 241 2,N-Dicyclohexyl-2-(2-pyridin-2-yl-benzimidazolyl-1-yl)-acetamide Similar to Example 140, pyridinic acid, cyclohexanefurfural, isocyanide Cyclohexane and N_t-butoxycarbonylphenylenediamine. MS (ES+): 417 (M+H). Example 242 121967.doc -144- 200811112 2,N-Dicyclohexyl_2-decylamine [2_(6-methyl-pyridyl)-benzimidazolylethyl, methylnicotinic acid, cyclohexanefurfural , isocyanocyclohexane and Ν-篦 dibutyl hydrazine # monobutoxycarbonyl phenylenediamine. MS (ES + ) ·· 431 (M+H) 〇Example 243 2,N-Dicyclohexyl_2_『2 V (3-methylpyridin-2-yl)-benzimidazole-1-yl b The indoleamine is similar to the example 14〇, 1 field A must be 1 methyl group in alkali acid, cyclohexane formaldehyde, isocyanide cyclohexane and hydrazine-: r: 丁 甘, 仙社# 一 虱 虱 carbene benzene Diamine. MS (ES + ) : 431 (M+H) 〇 Example 244 2,N-cyclohexyl n (6-fluorenylbenzo benzoyl 4 yl) acetamide is similar to κ, 140, 6-methylpicolinic acid , cyclohexanecarboxaldehyde, hexyl cyanide and N-tert-butoxycarbonyl stupid diamine. MS (ES+): 43 丄 (M+H) 〇 Example 245 2-[2-(2-Amino) · Pyridyl)-benzimidazole small group]_2,N-dicyclohexylacetamide/, similar to Example 140, 2-amino nicotinic acid, cyclohexane furfural, isopropyl decyl hydride and N - second butoxycarbonylphenylenediamine. ms (ES + ) ·· 432 (M+H) 〇 Example 246 121967.doc -145- 200811112 2-[2-(6•Cyano-n-bipyridine-3 -yl)-benzimidazol-1yl]-2,N-dicyclohexyl-acetamide similar to Example 140, 6-cyanonicotinic acid, cyclohexanecarbaldehyde, isocyanide cyclohexane and N - tert-butoxycarbonylphenylenediamine MS (ES+) · 442 (M+H). Example 247 2,N-dicyclohexyl 2 -[2·(2-methoxypyridin-3-yl) )-benzimidazole-1_yl]·Ethylamine is similar to Example 140, 2-methoxynicotinic acid, cyclohexane formaldehyde, isocyanocyclohexane and hydrazine-tert-butoxycarbonylbenzene Amine.ms (ES + ) : 447 (M+H). Example 248 gas _6_methyl·mouth ratio bite base)-benzoxanthene small group]_2, Ν·dicyclohexyl-acetyl amide is similar to Example 140, 2-gas _6_mercapto nicotinic acid, cyclohexane formaldehyde , isocyanocyclohexane and hydrazine-tert-butoxycarbonyl phenylenediamine. MS (ES+) ·· 466 (M+H) 〇Example 249 2-[2_(2_氱_6_methyl-pyridine_4_yl)_benzimidazole β1_ kib 2,N-dicyclohexyl ·Ethylamine

Similar to Example 140, 2-chloro-6-methyl acridine-4-carboxylic acid, cyclohexaneformaldehyde, isocyanatocyclohexane, and N-t-butoxycarbonylphenylenediamine. MS (ES + ) : 466 (M+H) 〇 Example 250 121967.doc -146- 200811112 2,N-Dicyclohexyl-2-(2-quinolin-3-yl-benzimidazolyl)_acetamidine The amine was similar to Example 140, porphyrin-3-carboxylic acid, cyclohexanecarboxaldehyde, isocyanocyclohexane and hydrazine-tert-butoxycarbonylphenylenediamine. MS (ES+): 467 (M+H) 〇 Example 251 2, N-dicyclohexyl-2-(2-quinolin-4-yl-benzimidazole q-yl-polyacetamide is similar to Example 140, 啥Lin-4-carboxylic acid, cyclohexane carboxylic acid, iso cyanide cyclohexane and N_t-butoxycarbonyl phenylenediamine. ms (ES+): 467 (M+H). Example 252 2-[2-( 3-Oxo-4-difluoromethyl-phenyl)-benzoxanthene-1-yl]_2,^_dicyclohexyl-acetamide is similar to Example 140, 3-chloro-4-yl-trifluoromethyl _benzoic acid, cyclohexanecarboxylic acid, iso-cyanylcyclohexane and N-tert-butoxycarbonylphenylenediamine.ms (ES+): 519 (M+H). Example 253 (S)-2-[2 -(4-Gas-phenyl-benzimidazole-; 1-kib-4-methyl-pentanoic acid cyclohexyl decylamine is similar to Example 140, 4-chlorobenzoic acid, isovaleraldehyde, isocyanide cyclohexane Alkyl and N-tert-butoxycarbonylphenylenediamine. MS (ES+): 424 (M+H). Example 254 2-(4-chloro-phenyl)-2-[2-(4-nitrogen) Phenyl)-benzimidazol-1-yl b-N-cyclohexyl-acetamide is similar to Example 140, 4-chlorobenzoic acid, 4-chlorobenzaldehyde, isocyanide ring 121967.doc -147- 200811112 And N-t-butoxycarbonylphenylenediamine.ms (ES + ) : 479 (M+H). Example 255 2-[2-(4-gas- Benzimidazole small group]_N•cyclohexyl-2-(4-trifluoromethyl-phenyl)-ethenylamine is similar to Example 140, 4-chlorobenzoic acid, 4-(trifluoromethyl)benzofural , isocyanocyclohexane and N_t-butoxycarbonylphenylenediamine. MS (ES + ) : 512 (M+H) 〇 Example 256 2·[2-(4-Gasyl)phenylene And carbazole+yl]_N_cyclohexyl_2_(3,4·diphenyl)-acetamide is similar to Example 140 in cyclohexane and N-t-butoxycarbonylphenylenediamine (M+H) Example 257 Cardiochlorobenzoic acid, 3,4-dichlorobenzaldehyde, isocyanation. MS (ES+) ·· 514 [2 (4 phenyl)-stupid and salivin-1-yl]cyclohexyl-2 -(3-Methoxy-phenyl)-acetamide similar to Example 140 for cyclohexane and N-(M+H) 〇 Example 258 'Bucking benzoic acid, 3-methoxybenzoquinal aldehyde , isocyano-butoxycarbonyl stupid diamine. MS (ES+) : 474 2-[2_(4_gas-phenyl bupidinoindol-1-yl)·Ν-cyclohexyl_2_pair Tolyl-B is similar to Example 140 in the form of 4-chlorobenzoic acid, p-tolualdehyde, isocyanatocyclohexane 121967.doc 200811112 alkane and N-t-butoxycarbonylphenylenediamine. ms (ES+): 45 8 (M +H). Example 259 2-[2-(4-Hydroxy-phenyl)-benzoxazole small base N-cyclohexyl-2-(3-carbo-phenylethylamine similar to Example 140, 4-chlorobenzene Formic acid, 3-fluorobenzaldehyde, isocyanocyclohexane and N-tert-butoxycarbonylphenylenediamine. ms (ES+): 462 (M+H) 〇 Example 260 2_[2-(4-gas _Phenyl)-benzimidazole_1-yl]_]&gt;^cyclohexyl_2_(4-difluoromethoxy-phenyl)-acetamide is similar to Example 140, 4-chlorobenzoic acid, II Fluoromethoxy)benzaldehyde, isocyanocyclohexane and N-tert-butoxycarbonylphenylenediamine. Ms (ES + ): 5 10 (M+H). Example 261 2-[2-(4-Hydroxy-phenyl)-benzimidazolyl]N-cyclohexyl-2_(2,5•difluoro-phenyl)-ethonamide similar to Example 140, 4-chloro Benzoic acid, 2,5-difluorobenzaldehyde, isocyanated % hexane and N-tert-butoxycarbonyl phenylenediamine. Ms (ES + ) : 480 (M+H) 〇 Example 262 2-[2-(4-Gas-phenyl)_ benzoimidazolyl N_cyclohexyl_2_(2_fluoro_5_methoxy -Phenyl)-acetamide Example 140 is similar, 4-chlorobenzoic acid, 2-fluoro-5-methoxybenzaldehyde, "Cyanide % hexane and N_T-butoxycarbonylphenylenediamine Ms (es+) ·· 121967.doc -149- 200811112 492 (M+H) 0 Example 263 (S)_2-[2-(5-Gas-2-fluorophenyl)_benzopyranoquinone_ι_ Keb 2,N_dicyclohexyl_acetamide is similar to Example 140 as '5-chloro-2-fluorobenzoic acid, cyclohexanone, heterocyclic cyclohexane and N-tert-butoxycarbonylbenzene Diamine MS (ES+): 469 (M+H). Example 264 (S)-2,N-dicyclohexyl-2-[2-(2,3-dimethoxy-phenyl)-benzo Imidazolyl]-Ethylamine is similar to Example 140, 2,3-dimethoxybenzoic acid, cyclohexanecarbaldehyde, isocyanocyclohexane and N-tert-butoxycarbonylphenylenediamine. ES + ) : 476 (M+H). Example 265 (S)-2_[2-(3_Ga-4-methoxy-phenyl)-benzo-salt-supplied 2,N-dicyclohexyl - acetamamine is similar to Example 140, 3-chloro-4-methoxybenzoic acid, cyclohexylcarbamate, isocyanocyclohexanone, and N-third butoxide Carbonyl phenylenediamine.ms (ES+) ·· 480 (M+H). Example 266 (S)-2-cyclohexyl-2-[2-(2,4-dimethoxy-phenyl)-benzo Imidazole-; 1-kib N_(2,6-dimethyl-phenyl)-acetamide

Similar to Example 140, 2,4-dimethoxybenzoic acid, cyclohexanecarbaldehyde, isocyanated 2,6-dimethylphenyl and N-tert-butoxycarbonylphenylenediamine. MS 121967.doc -150- 200811112 (ES + ) : 498 (M+H). Example 267 2-[2-(4-Gas-phenyl)-benzimidazole _;^基卜2•cyclohexyl, 'difluoro-cyclohexyl)-acetamide similar to Example 140, 4-chlorophenylhydrazine Acid, cyclohexane formaldehyde, i, μ difluoro 4-isocyano-cyclohexane and hydrazine-tert-butoxycarbonyl phenylenediamine. MS (ES + ): 486 (M+H). Example 268 (S)-2-[2-(4-Gas-phenyl)_benzimidazole_1β-yl]_2-cyclohexyl-7-diphenyl-difluoro-cyclohexyl)-ethenylamine is similar to Example 140. 4-gas benzoic acid, cyclohexane formaldehyde, difluoro 4-isocyano-cyclohexane, and pipedt-butoxycarbonylphenylenediamine. Ms (ES + ) : 486 (M+H). Example 269 (S)-2-[2-(2_Amino-pyridine-3-ylbendimidazolyl 2,N-dicyclohexyl-acetamide) Similar to Example 140, 2-aminonicotinine Acid, cyclohexanecarboxaldehyde, isocyanocyclohexane and N-tert-butoxycarbonylphenylenediamine. MS (ES+): 432 (M+H). Example 270 2,N-dicyclohexyl-2 -(6-Fluoro-2-pyridin-2-yl-benzimidazol-1-yl)-acetamide is similar to Example 140, picolinic acid, cyclohexanefurfural, isocyanocyclohexane and (2_ Amino- 4-fluoro-phenyl-p-aminocarbamic acid tert-butyl ester. MS (ES+): 432 (M+H) 〇121967.doc -151 - 200811112 Example 271 2,N-dicyclohexyl-2-[ 2-(2,4-dimethoxy-phenyl)_6-fluoro-benzimidazolyl]-acetamide is similar to Example 140 '2,4-dimethoxybenzoic acid, cyclohexane-formaldehyde, isocyanide Cyclohexane and (2-amino-4-fluoro-phenyl)-aminocarboxylic acid tert-butyl ester. (ES + ) : 494 (M+H). Example 272 2, N-dicyclohexyl-2 [6-Fluoro-2-(4-methoxy-phenyl)-benzimidazole small oxime is similar to Example 140, 4-methoxybenzoic acid, cyclohexane formaldehyde, isocyanatocyclohexane Burning and (2-amino-4-fluoro-phenyl)-aminocarboxylic acid third butyl vinegar MS (ES+): 464 (M+H). </RTI> </RTI> </RTI> <RTI ID=0.0></RTI> _ acetamide is similar to Example 140, 2,3-difluorobenzoic acid, cyclohexane formaldehyde, isocyanide cyclohexane and (2-amino-4-fluoro-phenyl)-carbamic acid third Butyl ester. MS (ES + ) : 470 (M+H). Example 274 2,N-dicyclohexyl-2-[2-(2,3-dimethoxy-phenyl)-6-fluoro-benzene And imidazol-1-yl]-acetamide is similar to Example 140, 2,4-dimethoxybenzoic acid, cyclohexanecarbaldehyde, isocyanocyclohexane and (2-amino-4-fluoro-benzene (3)-aminobutyric acid tert-butyl ester. MS (ES+): 494 (M+H). 121967.doc -152- 200811112 Example 275 2, cardinylcyclohexyl-2_[2_(2-ethyl-5) -Mercapto-2H_pyrazol-3-yl)-6-fluoro-benzo-flavor-1-yl]-ethanoamine similar to Example 140 ' 1 _ethyl-3 -fluorenyl _ 1H-吼峻-5 - formic acid, cyclohexane-burned formic acid, hetero-gasification, hexane and (2-amino-4-cyclo-phenyl)-aminocarboxylic acid tert-butyl ester. MS (ES + ) : 466 (Μ+ Η). Example 276 2,N-Dicyclohexyl_2-[2-(3,5-dimethyl-isoxazol-4-yl)_6_故·benzoxazol-1-yl]-B Indoleamine Example 14 0 is similar to '3,5-dimethylisoσ vomiting-4 - formic acid, cyclohexene, isopropyl emulsified, and (2-amino-4-fluoro-phenyl)-amino Second butyl phthalate. MS (ES + ) : 453 (Μ+Η). Example 277 2,N--cyclohexyl_2-[6_gas_2-(111-|| than 嗤-4_yl)_benzo-salt-1-yl] Ethylamine is similar to Example 140, 4 Pyrazolecarboxylic acid, cyclohexanecarboxaldehyde, heterocyclic cyclohexane and (2-amino-4-fluoro-phenyl)-carbamic acid tert-butyl ester. Ms (ES+) : 424 (Μ+Η) 〇Example 278 2,Ν-dicyclohexyl_2_[2_(1,5-dimethyl-1]3-pyrazolyl)_6_fluoro-benzo-anion- 1-yl]-acetamide is similar to Example 140, ^-dimethyl·1Η-pyrazole_3_carboxylic acid, cyclohexane formaldehyde, isocyanide cyclohexane, and (2_amino-4_fluoro) Phenyl)_t^ms(es+): 452 (m+h)0 soil (4) two 121967.doc -153- 200811112 Example 279 2,N-dicyclohexyl_2-[6_fluoro_2_(3• Methyl-isoxazole _5•yl)_benzimidazole·1- keb amide is similar to Example 140, 3-methyl-isoxazole _5_decanoic acid, cyclohexane formaldehyde, isocyanation Cyclohexane and (2-amino-4-fluoro-phenyl)-amino decanoic acid tert-butyl ester. MS (ES+): 439 (M+H). Example 280 2, Ν·dicyclohexyl_2-[6-fluoro-2-(111-pyrrolyl)·benzimidazolyl oxime

Similar to Example 140, pyrrole-2-carboxylic acid, cyclohexanecarboxaldehyde, isocyanocyclohexane and (2.Amino-4-fluoro-phenyl)-aminodecanoic acid tert-butyl ester. MS (ES + ): 423 (M+H). Example 281 2,N-Dicyclohexyl_2_[6-fluoro_2-(3-methyl-thienyl)-benzimidazole 1 yl]-ethanoamine similar to Example 140, 3-methyl-2- Thiophenecarboxylic acid, cyclohexanecarboxaldehyde, isocyanocyclohexane and (2-amino-4-fluoro-phenyl)-carbamic acid tert-butyl ester. MS (ES + ): 454 (M+H). Example 282 N-Phenylfluorenyl-2-[2-(4-carbophenyl)-benzimidazol-1-yl-2-ylcyclohexyl-acetamide is similar to Example 140, 4-phenoic acid, Cyclohexane formaldehyde, isocyanatobenzyl and N-tert-butoxycarbonylphenylenediamine. Ms (ES+): 458 (M+H) 〇121967.doc -154- 200811112 Example 283 N-butyl-2-[2-(4-gas-phenyl)_benzimidazole_1β-based 2_ ring Hexyl-acetamide is similar to Example 140, 4-chlorobenzoic acid, cyclohexanecarbaldehyde, isocyanatobutyl and N_t-butoxycarbonylphenylenediamine. Ms (ES+): 424 (M+H). Example 284 2-[2-(4-Gas-phenyl)-benzimidazole-1-ylbu]^-cyclohexyl-2-(tetrahydro-piperidin-4-yl)-acetamide and Example 140 Similarly, 4-chlorobenzoic acid, tetrahydro-bromic acid, isocyanocyclohexane and N-t-butoxycarbonylphenylenediamine. Ms (ES + ) : 452 (M+H) 〇 Example 285 2-[5-Gas-2-(4-Gas-phenyl)-6-fluoro-benzimidazolyl]_2,N-Dicyclohexyl_ Ethylamine is similar to Example 140, 4-chlorobenzoic acid, cyclohexanecarboxaldehyde, isocyanide cyclohexane, and (2-amino-5-chloro-4-fluoro-phenyl)-aminocarboxylic acid tert-butyl ester. (ES + ) : 503 (M+H) 〇 Example 286 2-[2-(4·Gas-phenyl)-5,6-difluoro-benzimidazole small group]々,~二环基基_ B The indoleamine is similar to the example 140, 4·chlorobenzoic acid, cyclohexanefurfural, isocyanide cyclohexane, and (2-amino-4,5-difluoro-phenyl)-amino decanoic acid tert-butyl ester. (ES + ) : 486 (M+H) 〇 Example 287 2-[2_(4_Chloro-phenyl)-benzopyrimidinyl 2b-cyclohexyl-good (tetrahydro-pyran - 121967.doc - 155 - 200811112 4-yl)-acetamide is similar to Example 140, 4·chlorobenzoic acid, cyclohexane formaldehyde, 4-isocyano-tetrahydro-pyran and N·t-butoxycarbonylphenyldiamine . MS (ES + ) : 452 (M+H) 〇 Example 288 2-[2-(4-Gas-phenyl)-benzimidazol-1-yl]_2-cyclohexyl_N-cyclopropyl-ethylhydrazine The amine was similar to Example 140, 4, benzoic acid, cyclohexanefurfural, isocyanatocyclopropane, and N.3 butyloxycarbonylphenylenediamine. MS (ES + ): 408 (M+H). Example 289 2,N-Dicyclohexyl-2-[2-(6-morpholin-4-yl-pyridin-3-yl)-benzimidazole_1-yl l-acetamide Similar to Example 140, 6-? Porphyrin nicotinic acid, cyclohexane formaldehyde, isocyanocyclohexane and N-tert-butoxycarbonylphenylenediamine. MS (ES + ) : 502 (M+H) 〇 Example 290 (S)-2-[2-(4-V-phenyl)-benzimidazol-1-yl]-2-cyclohexyl (tetrahydro- Piperaz-4-yl)-acetamide is similar to Example 140, 4-chlorobenzoic acid, cyclohexanecarboxaldehyde, 4-isocyano-tetrahydro-pyran and N-tert-butoxycarbonyl stupid diamine . MS (ES + ) ·· 452 (M+H) 〇 Example 291 (S)-2,N-Dicyclohexyl-2-[2-(4·methanesulfonyl-phenyl)-benzimidazole-1 - 121967.doc -156- 200811112 The carbamide is similar to the example 140, 4-(methylsulfonyl)benzoic acid, cyclohexanecarbaldehyde, isocyanocyclohexane and N-tert-butoxy Carbonyl phenylenediamine. Ms (ES+): 494 (M+H). Example 292 (S)_2-[2-(4-Gas-phenyl)-benzimidazolyl 2-cyclohexyl-N-cyclopropyl-acetamide Similar to Example 140, 4-chlorobenzoic acid, Cyclohexane formaldehyde, isocyanocyclopropane and N-tert-butoxycarbonylphenylenediamine. MS (ES+): 408 (M+H). Example 293 2·[6-Gas-2-(4-Gas-phenyl)-5-fluoro-benzimidazole_Kipbu·cyclohexyl (tetrahydro-pyran-4-yl)-acetamide Example 140 is similar, 4-gas benzoic acid, tetrahydro-pyran-4-formaldehyde, isocyanated % hexane, and (2-amino-4-chloro-5-fluoro-phenyl)-aminocarboxylic acid third Butyl ester. MS (ES + ) : 505 (Μ+Η) 〇Example 294 (S)-2-[2-(4·Ga-phenyl)_benzimidazole small group]_N_Cyclohexyl_2_(Tetrahydrogen Brigade Ethyl-4-yl)-ethinylamine is similar to Example 140, 4-oxobenzoic acid, tetrahydro-pyran-4-formaldehyde, isocyanocyclohexane and N-tert-butoxycarbonylphenylenediamine . Ms (ES+): 452 (M+H) 〇Example 295 (s)_2-[6-gas_2-(4_gasphenyl)_5_fluoro-benzo-salt-small-cyclohexyl·121967.doc - 157· 200811112 2-(Tetrahydro-piperidin-4-yl)-acetamide is similar to Example 140, 4-chlorobenzoic acid, tetrahydro-pyran-4-carbaldehyde, isocyanide cyclohexane and (2 -Amino-4-chloro-5-fluoro-phenyl)-tert-butyl carbamic acid. MS (ES + ) ·· 505 (M+H) 〇 Example 296 (S)-2-[2_(4-Gas-phenyl)-5,6-difluoro-benzimidazol-1-yl]_2, N-dicyclohexyl-acetamide is similar to Example 140, 4-chlorobenzoic acid, cyclohexane formaldehyde, isocyanide cyclohexane, and (2-amino-4,5-difluoro-phenyl)- Tert-butyl carbamic acid. MS (ES + ) ·· 487 (M+H) 〇Example 297 (S)-2_[2_(5 - gas-express-2-yl)-benzoxanthene-1 ·yl]- 2,N - Dicyclohexyl-acetamide is similar to Example 140, 5-chlorothiophene-2-decanoic acid, cyclohexanefurfural, isocyanatocyclohexane, and N-t-butoxycarbonylphenylenediamine. MS (ES+): 456 (M+H). Example 298 (S)-2,N-Dicyclohexyl_2-[2·(2,3-difluoro-phenyl)-6-fluoro-benzimidazol-1-yl]-acetamide and Example 140 Similarly, 2,3-difluorobenzoic acid, cyclohexanecarbaldehyde, isocyanatocyclohexane and (2-amino-4-fluoro-phenyl)-carbamic acid tert-butyl ester. MS (ES + ) ·· 470 (M+H). Example 299 2-[6-Gas-2-(4-Gas-phenyl)-5-fluoro-benzimidazole-1-yl]-N-cyclohexyl-2-cyclo 121967.doc -158- 200811112 pentyl _ 乙丑胺

Similar to Example 140, 4-chlorobenzoic acid, cyclopentane formaldehyde, isocyanocyclohexane and (2-amino-4-chloro-5-fluoro-phenyl)-aminocarboxylic acid tert-butyl ester. MS (ES + ): 489 (M+H). Example 300 (8)-2-[6_Gas-2-(4-chloro-phenyl)-5-fluoro-benzo-en- ol-1-yl]-heptanoic acid cyclohexyl decylamine is similar to Example 140, 4 -Chlorobenzoic acid, hexanal, isocyanide cyclohexane and (2-amino-4-chloro-5-fluoro-phenyl)-carbamic acid tert-butyl ester. MS (ES + ): 491 (M+H). Example 301 (S)-2-[6-Gas-2-(4-Gas-phenyl)-5-fluoro-benzimidazol-1-yl]-indole-cyclohexyl-2-cyclopentyl-acetamidine The amine was similar to Example 140, 4-chlorobenzoic acid, cyclopentanecarboxaldehyde, isocyanocyclohexane and (2-amino-4-chloro-5-fluoro-phenyl)-carbamic acid tert-butyl ester. Ms (ES+): 489 (M+H) 〇 Example 302 2-[2-(4-Gas-phenyl)-5-fluoro-benzimidazol-1-yl]-2,N-Dicyclohexyl-B The guanamine was added to 4-hexane benzoic acid (156.6 mg, 1 mmol, 1 eq.) to cyclohexane decanoic acid (168_3 mg, 1.5 mmol, 1.5 eq.), hexanes (109.2 g, 1 mmol, 1 Equivalent) and (2-amino-5-fluoro-phenyl)-carbamic acid diisopropylidene (210.2 mg '1 mmol, 1 eq.) in methanol (15 mL) Stir under 16 hours. The solvent was evaporated and the crude product was extracted from acetic acid &lt;RTI ID=0.0&gt;&gt; After separating the organic layer and evaporating the solvent, the residue was dissolved in acetonitrile. Mulin (435.5, 5 mmo, 5 equivalents) and hydrazine (triphenylphosphine)|ii (23 limg, 〇.2 匪〇1, 〇·2 eq.) were added and the mixture was stirred at room temperature for 3 hours. The solvent was evaporated and the crude product was extracted in the night from ethyl acetate and NaHC. After separating the organic layer and evaporating / granules, the residue was dissolved in acetic acid. The mixture was at 8 Torr. Stir under the arm for 16 hours. The solvent was evaporated and the product was isolated via preparative hPLC. MS (ES+) · · 469 (M+H) 〇 Example 303 2-[1-(cyclohexyl-cyclohexylaminecarbazyl-methyl)-5,6-difluoro-1 fluorene-benzimidazole-2- Methyl phenyl benzoate is similar to Example 140, monomethyl phthalate, cyclohexane formaldehyde, isocyanocyclohexane and (2-amino-4,5-difluoro-phenyl)-amine Tert-butyl carboxylic acid. MS (ES + ) : 510 (Μ+Η). Example 304 2,]^-Dicyclohexyl-2_(5,6-difluoro-2_.pyridin-2-yl-benzofuran-1-yl)-acetamide Similar to Example 140, hexahydrogen Pipec〇iic acid, cyclohexane formaldehyde, isocyanide cyclohexane and (2-amino-4,5-difluoro-phenyl)-carbamic acid tert-butyl ester. MS (ES + ): 453 (M+H). Example 305 2-[2-(5-Gas-隹-phen-2-yl)-5,6-di-benzo-indole-1-yl]-2,]\_dicyclohexyl-acetamide Example 140 is similar, 5-chlorothiophene-2-carboxylic acid, cyclohexane formaldehyde, isocyanide 121967.doc • 160- 200811112 cyclohexane and (2-amino-4,5-difluoro-phenyl)-amine Tert-butyl carboxylic acid. MS (ES + ): 493 (M+H). Example 306 2-[6-Gas-1-(cyclohexyl-cyclohexylaminecarbazyl-methyl)-5-fluoro-1H-benzoimidazol-2-yl]-benzoic acid methyl ester was similar to Example 140. Monomethyl phthalate, cyclohexane formaldehyde, isocyanide cyclohexane and (2-amino-4-chloro-5-fluoro-phenyl)-carbamic acid tert-butyl ester. MS (ES+) ·· 526 (M+H). Example 307 2_(6·Ga-5·Fluoro-2-pyridin-2-yl-benzimidazolyl-1-yl)-2,N-dicyclohexyl-acetamide Similar to Example 140, hexahydrotobacillus Acid, cyclohexane formaldehyde, isocyanide, and (2-amino-4-chloro-5-fluoro-phenyl)-aminocarboxylic acid tert-butyl ester. MS (ES +) · 4 6 9 ( +Η) 〇Example 308 2-(6-gas-5_fluoro-2-port ratio -3-yl-benzoate, hydrazine small group)-2, Ν二Cyclohexyl·acetamide is similar to Example 140, nicotinic acid, and (2-amino-4-gas-5-fluoro-phenyl(ES+)·· 469 (Μ+Η). Example 309

Cyclohexane formaldehyde, isocyanide cyclohexane) - tert-butyl carbamic acid. MS benzoimidazol-1-yl)-2,N-dicyclohexyl-2-(6-a-5-fluoro-2-pyridyl-4-ylacetamide is similar to the example 140 in acid, cyclohexane Formaldehyde, isocyanide cyclohexane 121967.doc • 161 - 200811112 and (2-amino-4-chloro-5-fluoro-phenyl)-carbamic acid tert-butyl vinegar. ms (ES+) : 469 (M +H). Example 310 2-[6-Gas_2_(3_Gas-Phenyl-2-yl)-5-fluoro-benzoxanthene-1-yl-2-N-dicyclohexyl-acetamide Similar to Example 140, 3-chlorothiophene-2-carboxylic acid, cyclohexane methyl ester, heterocyclic cyclohexane, and (2-amino-4-chloro-5-fluoro-phenyl)-carbamic acid third MS (ES + ) : 509 (M+H). Example 311 2-[6_Gas_2_(5_Gas_Sp.2_base)_5_Gasbenzo-嗤_1ββ-based] _2,N-Dicyclohexyl-acetamide is similar to Example 140, 5-chlorothiophene-2-carboxylic acid, cyclohexanecarbaldehyde, isocyanide cyclohexane, and (2-amino-4-gas-5-fluoro -phenyl)-tert-butyl carbamic acid tert-butyl ester MS (ES + ) : 509 (M+H). Example 312 (S)-2-[6- gas-2 _(4- s-phenyl)- 5-Fluoro-benzimidazole β1-kibethylpentanoic acid cyclohexyl decylamine is similar to Example 140, 4-chlorobenzoic acid, 2-ethylbutyraldehyde, isocyanide cyclohexane And (2-amino-4-chloro-5-fluoro-phenylaminocarboxylic acid tert-butyl ester.

0 MS (ES+) ·· 491 (M+H) 实例 Example 313

Acetylcyclohexane formaldehyde, isocyanide ring similar to Example 140, 4·fluorobenzoic acid, 121967.doc -162- 200811112 hexane and (2-amino-4-chloro-5-fluoro-phenyl) - tert-butyl carbamic acid. MS (ES + ) : 491 (M+H) 〇 Example 314 2-[2-(4-Gas-phenyl)-benzoxime-1 -yl]_2-cyclohexyl-N-(l-isopropyl -2-Methyl-propyl)-ethnamine is similar to Example 140, 4-chlorobenzoic acid, cyclohexane formaldehyde, 1-isopropyl-2-mercaptopropane and N-tert-butoxy Carbophenylene diamine. MS (ES + ): 466 (M+H). Example 315 2-[6-Gas-2-(4- gas-phenyl)-5. gas-benzo-flavor-l-yl]-2-cyclohexyl-N-cyclopentyl-acetamide and examples 140 is similar to 4-chlorobenzoic acid, cyclohexanecarbaldehyde, isocyanatocyclopentane and (2-amino-4-chloro-5-fluoro-phenyl)-carbamic acid tert-butyl ester. MS (ES + ): 489 (M+H). Example 316 2-[2_(4_Gas-phenyl)-5,6-digas* _benzoxanthene-1 -yl]-N-cyclohexyl_2-(tetrazine-transfero-4-yl -Ethylamine is similar to Example 140, 4-oxobenzoic acid, tetrahydro-pyran-4-carbaldehyde, isocyanurized hexazone and (2-amino-4,5-difluoro-phenyl)- The third carboxylic acid formic acid is intended. MS (ES + ): 488 (M+H). Example 317 (S)-2-[2-(4-Gas-phenyl)-5-fluoro-benzimidazole-1·yl]·2, fluorenyl-dicyclohexyl-acetamide is similar to Example 302, 4 - chlorobenzoic acid, cyclohexane formaldehyde, isocyanide ring 121967.doc • 163- 200811112 Hexane and (2-amino-5-fluoro-phenyl)-carbamic acid allyl ester. Ms (ES + ): 468 (M+H) 〇 Example 318 2-[2-(4-Gas-phenyl)_5,6-difluoro-benzimidazole-1_ kib 2_cyclohexyl_Ν- (Tetrahydro-Brain-4-yl)·Ethylamine is similar to Example 140, 4-chlorobenzoic acid, cyclohexaneformaldehyde, decarboxylated-tetrahydro-pyran and (2-amino-4, 5-Difluoro-phenyl)-aminocarboxylic acid tert-butyl. MS (ES+): 489 (Μ+Η). Example 319 2_[6_Gas-2-(4-Gayl-phenyl)-5-fluoro-benzimidazole small group]-2-cyclohexyl I (tetrahydro-l-butanyl-4-yl)-acetamide Similar to Example 140, 4-chlorobenzoic acid, cyclohexane formaldehyde, 4-isocyano-tetrahydro-pyran and (2-amino-4-chloro-5-fluoro-phenyl)-aminocarboxylic acid Tributyl ester. MS (ES + ): 505 (M+H). Example 320 2,N-Dicyclohexyl-h[2-(3-dimethylamino-phenyl)-5,6-difluoro-benzimid-1-yl]-acetamide is similar to Example 140 3 - dimethylaminobenzoic acid, cyclohexane methyl, isocyanocyclohexane and (2-amino-4,5-difluoro-phenyl)-aminocarboxylic acid tert-butyl ester. MS (ES + ): 495 (M+H). Example 321 2,N-Dicyclohexyl 2 -[2_(3-dimethylaminophenyl)fluoro-benzimidazol-1-yl]-ethenylamine similar to Example 140, 3-dimethylamine Benzoic acid, cyclohexanecarboxaldehyde, 121967.doc -164- 200811112 Heterogasification %»hexane and (2-amino-4-fluoro-phenyl)-amino decanoic acid tertidine. MS (ES + ): 477 (M+H). Example 322 2-[2-(4-Gas-phenyl)-5,6-difluoro-benzimidazol-1-yl-2-cyclohexyl-]\[-(1-isopropyl-2-methyl Base-propyl)-acetamide is similar to Example 140, 4-chlorobenzoic acid, cyclohexanecarbaldehyde, isocyanato-1-isopropyl-2-mercaptopropane, and (2-amino-4,5- Difluoro-phenyl)-amino decanoic acid tert-butyl ester. MS (ES + ): 503 (M+H). Example 323 2-[6-Gas-2-(4-Gas-phenyl)-5-fluoro-benzimidazol-1-yl]-2-cyclohexyl-indole-(1-isopropyl-2-yl) The propyl-propyl)-acetamide is similar to the example 140, 4-chlorobenzoic acid, cyclohexanefurfural, isocyanide, isopropyl-2-methylpropane, and (2-amino-4-chloro -5-Fluoro-phenyl)-aminobutyric acid tert-butyl ester. MS (ES + ): 519 (M+H). Example 324 2-[2-(3-Gas-phenyl)·5,6·difluoro·benzoimin-1-yl 2,N-dicyclohexyl_acetamide is similar to Example 140, 3- Chlorobenzoic acid, cyclohexane formaldehyde, isocyanocyclohexane and (2-amino-4,5-difluoro-phenyl)-carbamic acid tert-butyl ester. Ms (ES+): 487 (M+H). Example 325 2-[2-(2·Ga·n-yl)-5,6-di-I-benzo-saltyl 2,N-dicyclohexylidene is similar to Example 140, 2-chlorophenylhydrazine Acid, cyclohexane formaldehyde, isocyanidation 121967.doc -165- 200811112 hexane and (2-amino-4,5-difluoro-phenylglycolic acid tert-butyl ester. MS (ES+). 487 (M+H) 〇 Example 326 (S)-2-[6_Ga-5-fluoro-2-(4-fluoro-phenyl-benzoxazole small group)·2,Ν-dicyclohexyl- Ethylamine is similar to Example 140, 4-fluorobenzoic acid, cyclohexanecarboxaldehyde, isocyanocyclohexane and (2-amino-4-chloro-5-fluoro-phenyl)-aminocarboxylic acid tert-butyl Ester. MS (ES+): 487 (M+H). Example 327 (S) -2-[2-(4---phenyl-phenyl)-5,6-difluoro-benzo-benzo-l-yl]- N-cyclohexyl-2_(tetrahydro-pyran-4-yl)-acetamide is similar to Example 140, 4-chlorobenzoic acid, tetrahydro-pyran-4-carbaldehyde, isocyanocyclohexane and 2_Amino-4,5-difluoro-phenyl)-aminocarboxylic acid tert-butyl ester MS (ES + ) ·· 488 (M+H). Example 328 2-[2-(4- gas- Phenyl)-5-fluoro-benzimidazol-1-yl]cyclohexyl-2-(tetrahydro-pyran-4-yl)-acetamide is similar to Example 302, 4·chlorobenzoic acid, tetrahydrogen -piperidin-4- Aldehyde, isocyanocyclohexane and (2-amino-5-fluoro-phenyl)-aminocarboxylic acid allyl ester. MS (ES+): 470 (M+H) 〇 Example 329 2-[2_(4 - gas-phenyl)_6_fluoro·benzimidazole•yl]_N-cyclohexyl-2-(tetrazole-piperidin-4-yl)-acetamide similar to Example 140, 4-chlorobenzoic acid, Tetrahydro-piperidin-4-carbaldehyde, isogas 121967.doc -166 - 200811112 cyclohexane and (2-amino-4-fluoro-phenyl)-amino decanoic acid terpene vinegar ° MS (ES+ 470 (M+H). Example 330 2-[2-(4-Gas-phenyl)-6-fluoro-benzimidazol-1-yl]-N-cyclohexyl Ktetrazole-pyran- 2-yl)-acetamide is similar to Example 140, 4-chlorobenzoic acid, tetrahydro-pyran-2-methyl, iso-gasified cyclohexane, and (2-amino-4-fluoro-phenyl) )-Aminoacetic acid terpene vinegar ° MS (ES + ) ·· 470 (M+H) 〇Example 331 2-[6-Gas-2-(4-Ga-phenyl)_5-fluoro-benzimidazole _;[•Kib N-cyclohexyl_2-(tetrahydro-piperidin-2-yl)-acetamide is similar to Example 140, 4-oxobenzoic acid, tetrahydro-pyran-2-carbaldehyde, iso Cyanated %1 hexane and (2-amino-4-chloro-5-fluoro-phenyl)-aminocarboxylic acid tertidine. MS (ES + ) : 505 (Μ+Η). Example 332 (S)-2,N-Dicyclohexyl-2-[6-fluoro-2_(3·methyl·thienylbenzimidazole-1-yl)-ethenylamine is similar to Example 140, 3-A Base-2-nonporous carboxylic acid, cyclohexane carboxylic acid, isocyanocyclohexane and (2-amino-4-fluoro-phenyl)-amino phthalic acid tert-butyl ester. MS (ES+): 454 ( M+H) 〇Example 333 (8)2-[2-(2-Ga-Benzyl)-5,6-difluoro-benzopyrimidin-1-yl 2,]^-Dicyclohexyl-B The amine is similar to Example 140, 2-chlorobenzoic acid, cyclohexane formaldehyde, isocyanide ring 121967.doc -167- 200811112 hexane and (2-amino-4,5-difluoro-phenyl)β amine Tert-butyl carboxylic acid. MS (ES+): 487 (M+H). Example 334 (S)-2-[2-(4- s-phenyl)-5-fluoro-benzimidazolyl cyclohexyl 2彳Tetrahydro-piperidin-4-yl)-acetamide is similar to Example 302, 4-chlorobenzoic acid, tetrahydro-pyran-4-carbaldehyde, iso-cyanide hexane and (2-amino-) 5-fluoro-benzyl)-------- MS (ES + ): 470 (M+H). Example 335 (S)-2-[2_(4- gas-phenyl)-6-fluorobenzoyl-indole-1_yl]cyclohexyl-2-(tetrahydro-pyran-4-yl)-B The guanamine is similar to Example 140, 4-chlorobenzoic acid, tetrahydro-piperidinaldehyde, isocyanocyclohexane, and (2-amino-4-fluoro-phenyl)-amino decanoic acid tert-butyl ester. MS (ES + ): 470 (M+H). Example 336 (S)-2-[2-(4-Gas-phenyl)_6_benzopyranyl Nb-N-cyclohexyl-2-(R)-tetrahydropyranyl I-acetamide Example 140 is similar to chlorobenzoic acid, tetrahydro-pyran-2-daldehyde, isocyanatocyclohexane, and (2-amino-4-fluoro-phenyl y-aminodecanoic acid tert-butyl ester. MS ( ES + ) : 470 (M+H) 〇Example 337 (S) -2-[2-(4-Gas-Phenyl 6-Mouse_Benzene Miso Small Substrate...Cyclohexyl-2-(S) -Tetrahydropyranyl-2-yl-acetamide is similar to Example I40, chloroformic acid, tetrahydro-pyran-2-carbaldehyde, isocyanide 121967.doc 200811112 cyclohexane and (2-amino- 4-Fluoro-phenyl)-tert-butyl methacrylate, MS (ES+): 470 (M+H). Example 338 2-[2-(4-carbo-phenyl)-5-fluoro-benzo Imidazolyl-1-yl]-yicyclohexyl-2(tetrahydropiperidin-2-yl)-acetamide is similar to Example 302, 4-chlorobenzoic acid, tetrahydro-piperidinaldehyde, isocyanide cyclohexane Alkane and (2-amino-5-fluoro-phenyl)-carbamic acid allyl _ ° MS (ES + ): 470 (M+H). Example 339 2,N-dicyclohexyl-2-[2 -(3,4-dioxa-phenyl)-6-methoxy-benzimidazol-1-yl]-acetamide is similar to Example 140, 3,4-dibenzoic acid, cyclohexanecarbaldehyde, different Cyanide cyanide and (2-amino-4-methoxy-phenyl)-carbamic acid tert-butyl ester. MS (ES+): 514 (M+H). Example 340 2-[2-( 4-oxo-phenyl)-6-methoxy-benzimidazol-1-yl]-2,N-dicyclohexyl_ethonamide

Similar to Example 140, 4-chlorobenzoic acid, cyclohexanecarboxaldehyde, isocyanocyclohexane and (2-amino-4-methoxy-phenyl)-carbamic acid tert-butyl vinegar. MS (ES + ): 480 (M+H). Example 341 2-[2-(5-Gaxo-indolyl)-6-methoxy-benzoxanthene-1-yl b 2,N-dicyclohexyl·ethinylamine similar to Example 140, 5- Chloro-σ-cetin-2-carboxylic acid, cyclohexanone, isocyanide 121967.doc -169- 200811112 cyclohexane and (2-amino-4-methoxy-phenyl)-carbamic acid Three vinegar. MS (ES + ) : 486 (M+H) 〇 Example 342 2_[2-(3-Ga-4-methoxy-phenyl)-6-methoxy-benzopyranyl^,... Cyclohexyl-acetamide is similar to Example 140 in the form of '3-chloro-4-methoxybenzoic acid, cyclohexanone, iso-cyclohexane, and (2-amino-4-methoxy-phenyl) ) - tert-butyl carbamic acid. MS (ES+): 510 (M+H). Example 343 2-[2-(4-Gas-3-fluoro-phenyl)-6-methoxy-benzoxanthene-1-yl b 2,N-dicyclohexyl-ethenylamine similar to Example 140 4-cyclo-3-fluorobenzoic acid, cyclohexanefurfural, isocyanide cyclohexane and (2-amino-4-methoxy-phenyl)-carbamic acid tert-butyl ester. MS (ES + ): 498 (M+H). Example 344 2-Cyclohexyl-N-cyclopentyl-2-[2-(3,4-dioxa-phenyl)-6-methoxy-benzimidazol-1-yl]-acetamide with Example 140 Similarly, 3,4-dibenzoic acid, cyclohexanecarbaldehyde, isocyanatocyclopentane and (2-amino-4-methoxy-phenyl)-carbamic acid tert-butyl ester. MS (ES + ) : 500 (M+H) 〇 Example 345 N-cyclohexyl-2-cyclopentyl-2-[2-(3,4_di-phenyl)-6-methoxy-benzo Imidazol-1-yl]-acetamide is similar to Example 140, 3,4-dichlorobenzoic acid, cyclopentane formaldehyde, isocyanide 121967.doc -170- 200811112 cyclohexane and (2-amino-4 -Methoxy-stupyl)-tert-butyl amide. MS (ES + ) : 500 (M+H) 〇 Example 346 -^-... gas-phenyl "-methoxy-benzopyrene + yl-cyclohexyl Cyclopentyl acetamide and examples Similar to 140, 4-gas benzoic acid, cyclohexane formaldehyde, isocyanatocyclopentane and (2-amino-4-methoxy-phenyl)-amino decanoic acid tert-butyl ester. MS (ES + ·· 466 (M+H). Example 347 2_[2_(3_--phenyl)-6-methoxybenzimidazole small base 2,N-dicyclohexyl·acetamide is similar to Example 140 , 3-chlorobenzoic acid, cyclohexane formaldehyde, isocyanatocyclohexane and (2-amino-4-methoxy-phenyl)-aminocarboxylic acid tert-butyl. MS (ES + ): 480 (M+H) 〇 Example 348 2,N-Dicyclopentyl-2-[2-(3,4-di-phenyl)-6-methoxy-benzimidazol-1-yl]- The acetamide is similar to the example 140, 3,4-dibenzoic acid, cyclopentane formaldehyde, isocyanatocyclopentane and (2-amino-4-methoxy-phenyl)-carbamic acid third Butyl ester. MS (ES + ) : 486 (M+H) 〇 Example 349 2-[2-(4- gas-phenyl)-6-methoxy-benzo-indole-1-yl]-N- Cyclohexyl-2-cyclopentyl-acetamide is similar to Example 140, 4-carbon benzoic acid, cyclopentane formaldehyde, isocyanide ring 1 21967.doc -171 - 200811112 Hexane and (2-amino-4-methyl-phenyl)-aminoformamidine terpene vinegar.ms (ES + ) ·· 466 (M+H). 350 2-[2-(4-Gas-3-fluoro-phenyl)_6_decyloxy-benzimidazole_1β-yl]_2-cyclohexyl·N-cyclodecyl-ethenylamine is similar to Example 140. 4-Chloro-3-fluorobenzoic acid, cyclohexanic acid, isocyanatocyclopentane and (2-amino-4-methoxy-phenyl)-carbamic acid tert-butyl ester. MS (ES+ ): 484 (M+H). Example 351 2-[2-(3-Vethoxymethoxy-phenyl)-6-methoxy-benzimidazole-1-yl]-2-cyclohexyl-N- Cyclopentyl-acetamide is similar to Example 140, 3-ox-4-methoxybenzoic acid, cyclohexanecarbaldehyde, isocyanatocyclopentane, and (2-amino-4-methoxy-phenyl) - 3-butyl carbamic acid ester. MS (ES+) · 496 (M+H). Example 352 2,N-dicyclohexyl-2-[2-(4.fluoro-phenyl)·6-A Oxy-benzimidazole-1_yl]·acetamide is similar to Example 140, 4-fluorobenzoic acid, cyclohexanefurfural, isocyanide cyclohexane, and (2-amino-4-methoxy) -Phenyl)-tert-butyl methacrylate. MS (ES + ) : 464 (M+H) 〇 Example 353 2-[2-(3-Gas-phenyl)·6-曱 Oxygen -Benzimidazol-1-yl]-2-cyclohexyl_N•cyclopentyl-ethenylamine similar to Example 140, 3-chlorobenzoic acid, cyclohexanefurfural, isocyanide ring 121967.doc - 172- 200811112 Pentane and (2-amino-4-methoxy-phenyl)-aminocarboxylic acid tert-butyl ester. MS (ES+) ·· 466 (M+H) 〇 Example 354 2-[2-(3-Gas-4-methoxy-phenyl)-6-decyloxy-benzopyran-1-yl] · Ν-cyclohexyl-2-cyclopentyl-ethrolamine similar to Example 140, 3-chloro-4-nonyloxybenzoic acid, cyclopentane formaldehyde, isocyanocyclohexane and (2-amino) T-butyl -4-methoxy-phenyl)-carbamic acid. MS (ES + ) : 496 (Μ+Η). Example 355 2-[2-(5-Chloro-thiophen-2-yl)-6-methoxy-benzimidazole-1.yl]cyclohexyl-2-cyclopentyl-acetamide The analogy was similar to Example 140. 5-Chloro-thiophene-2-carboxylic acid, cyclopentane formaldehyde, isocyanocyclohexane and (2-amino-4-methoxy-phenyl)-carbamic acid tert-butyl ester. MS (ES + ): 472 (M+H). Example 356 2-Cyclobutyl-N-cyclohexyl-2-indole 2-(3,4-dioxa-phenyl)-6-methoxy-benzoxazol_1-yl acetamide and examples 140 is similar to 3,4-dichlorobenzoic acid, cyclobutanecarbaldehyde, isocyanatocyclohexane and (2-amino-4-methoxy-phenyl)-carbamic acid tert-butyl ester. MS (ES + ) ·· 486 (M+H) 〇 Example 357 2-[2-(5-Gas-thiophen-2-yl)-6-methoxy-benzimidazol-1-yl b 2-ring Hexyl-N-cyclopentyl-acetamide is similar to Example 140, 5-chloro-thiophene-2-carboxylic acid, cyclohexanecarbaldehyde, isocyanide 121967.doc-173 - 200811112 cyclopentane and (2-amino) -4·decyloxy-phenyl)-amino citrate tributyl. MS (ES+): 472 (Μ+Η). Example 358 2_[2-(6-a-cyclopyridin-3,yl)-6-methoxy-benzoxazole small group]_2 '~Lycosyl-acetamide is similar to Example 140, 6-chloro - nicotinic acid, cyclohexanefurfural, decyl isocyanide and tert-butyl (2-amino-4-methoxy-phenyl)-aminocarbamate. (ES+) : 481 (M+H). Example 359 2-[2-(3-Gas-phenyl)-6-methoxy-benzimidazolyl]-N-cyclohexyl_2-cyclopentyl-acetamide is similar to Example 14 0 '3 - Gas benzoic acid, cyclopentanecarboxylic acid, isocyanocyclohexane and (2-amino-4-methoxy-phenyl)-aminocarboxylic acid tert-butyl ester. MS (ES + ): 466 (M+H). Example 360 2·[2-(3-Oxomethoxy-phenyl)-6-methoxy-benzimidazole+yl^,... Dicyclopentyl-acetamide is similar to Example 140, 3- gas- 4-methoxybenzoic acid, cyclopentane formaldehyde, isocyanatocyclopentane and (2.Amino-4-methoxy-phenyl)-aminocarboxylic acid tert-butyl ester. MS (ES + ) : 482 (M+H) 〇 Example 361 2,N-dicyclohexyl-2-[6-methoxy-2-(6-trifluoromethyl- butyl)-benzimidazole- 1-yl]-acetamide is similar to Example 140, 6-trifluorodecyl-final acid, cyclohexane carboxylic acid, iso 121967.doc -174- 200811112 cyanide cyclohexane and (2-amino-4 -Methoxy-phenyl)-tert-butyl methacrylate. MS (ES + ) : 515 (M+H) 〇 Example 362 2-[2-(5-Gas-thiophen-2-yl)-6-methoxy-benzimidazol-1-yl]-2-ring Butyl-N-cyclohexyl-acetamide is similar to Example 140, 5-chloro-thiophene-2-carboxylic acid, cyclobutanecarbaldehyde, isocyanocyclohexane and (2-amino-4-methoxy- Phenyl)-tert-butyl methacrylate. MS (ES+): 458 (M+H). Example 363 2-[2-(3-Gas-phenyl)-6-methoxy-benzimidazole-i-yl]-2.cyclobutyl-N-cyclohexyl-acetamide is similar to Example 140. 3-benzoic acid, cyclobutanecarbaldehyde, isocyanatocyclohexane and (2-amino-4-methoxy-phenyl)-aminocarboxylic acid tert-butyl ester. MS (ES + ): 452 (M+H). Example 364 N-cyclohexyl-2-cyclopentyl-2-[2-(4-fluoro-phenyl)-6-methoxy-benzimidazol-1-yl]-ethnamine was similar to Example 140. 4-fluorobenzoic acid, cyclopentane formaldehyde, isocyanocyclohexane and (2-amino-4-methyl-phenyl)-carbamic acid tert-butyl ester. Ms (ES + ) : 450 (M+H). Example 365 (2-Amino-4,5-difluoro-phenyl)-carbamic acid tert-butyl ester

Add 4,5-difluoro-2-nitrophenylamine (6·〇g, 34 mmol, 1 eq.) to monolithic acid-di-indole dibutyl S (14.8 g, 68 mmol, 2 eq.) And dm AP 121967.doc • 175-200811112 (211 mg, 0.2 mmol, 〇·05) in THF 〇〇〇 mL) and the mixture was stirred at room temperature for 72 hr. The solvent was evaporated and the crude product was extracted from ethyl acetate and aqueous NaHC. The residue was dissolved in dcm and cooled to o °c. Trifluoroacetic acid (7·75 g, 68 mm 〇 1, 2 eq.) was added slowly and the mixture was placed in hydrazine. (The mixture was stirred for 48 hours. 2 N Na〇H was added to remove the organic layer from the ?11 value to 7 knives and evaporated. The residue was dissolved in ethyl acetate and the product was extracted from aqueous NaHCCh. The intermediate was separated and dissolved. 4·28 g (16 mmol, ! eq) was dissolved in dmf (5 〇ml) and 13 ml of saturated NEUC1 solution was added. The powder (51 g, 78 mmol, 5 equivalents) was added and suspended. The solution was stirred at 80 °C for 3 hrs and then at room temperature for 2 hrs. The remaining solid was filtered and evaporated and evaporated and evaporated. 366 (2-Amino-4-fluoro-phenyl)-carbamic acid tert-butyl ester was similar to Example 365, starting from 4-fluoro-2-nitro-phenylamine. Example 367 (2-amine 4-Methoxy-phenyl)-carbamic acid terpene vinegar was similar to Example 365 starting from 4-decyloxy-2-nitro-phenylamine. Example 368 (2-Amino- 4 _Bromo-phenyl)-amino decanoic acid tert-butyl ester was similar to Example 365, starting from 4-bromo-2-nitro-phenylamine. Example 369 (2-Amino-4- gas-phenyl )-T-butyl carbamic acid 121967.doc -176- 200811112 Similar to Example 365, starting with 4-chloro-2-nitro-phenylamine. Example 370 (2-Amino-5- -4-fluorophenyl)-carbamic acid III Butyl ester was similar to Example 365, starting from 5-chloro-4-fluoro-2-nitro-phenylamine. Example 371 (2. Amino-4-ox-5-fluoro-phenyl)-carbamic acid The third butyl ester was similar to Example 365 starting from 4-chloro-5-fluoro-2-nitro-phenylamine. Example 372 (2-Amino-5-fluoro-phenyl)-amino decanoate Propyl ester (2-amino-4-fluoro-phenyl)-aminocarboxylic acid tert-butyl ester (5 〇g, 22 mmo, 1 equivalent) was added to DIpEA (3 62 m b 22 mni〇1, 1 equivalent The solution was stirred in THF (80 ml). The mixture was cooled to EtOAc EtOAc (EtOAc m. The solvent was evaporated and the crude product was extracted from ethyl acetate and aqueous NaHCO3. The residue was dissolved in dcm and trifluoroacetic acid (1·1) for 2 hours. The product was obtained after evaporation of organic solvent. Fluoro-4-isocyano-cyclohexane 4,4-mono-m-hexylamine hydrochloride (ι·〇g, 5.8 mmol, 1 equivalent Add to NaOH (1.5 g, 37 mmol, 6.3 eq.) and tetrabutylammonium hydrogen sulfate (40 mg, 0.12 mmol, 0.02 eq.) in water (2.5 ml), m. (3 ml, 3 7 mmol, -6 eq) And in a mixture of DCM (5 ml). The mixture was stirred at room temperature for 72 hours and the crude was extracted with DCM. The product was isolated by Kieslgel chromatography. Example 374 121967.doc • 177·200811112 4-Iso-l-yl-tetrahydro-traditional taste Similar to Example 373, starting from tetrahydro-pyran-4-ylamine. Example 375 Tetrahydro- σ 味 -2- -2- 将 乙 乙 ( 3.9 3.9 3.9 3.9 3.9 3.9 3.9 3.9 3.9 3.9 3.9 3.9 3.9 3.9 3.9 3.9 3.9 3.9 3.9 3.9 3.9 3.9 3.9 3.9 3.9 3.9 。 DMSO (3.7 g, 52 mmol, 2 eq.) in EtOAc (10 mL) was added dropwise and the mixture was stirred for 20 min. Tetrahydropyran-2-methanol (3 g, 26 mmol, 1 eq.) was dissolved in DCM (10 mL) and was added dropwise to the reaction mixture. After 15 minutes, triethylamine (18 ml) was added dropwise and the mixture was warmed to room temperature. Water was added and the crude product was extracted with DCM. The product was isolated by Kieselgel chromatography.

EXAMPLE A Film-coated lozenges containing the following ingredients can be made in a conventional manner: Ingredients Per tablet core: Compound of formula (I) 10.0 mg 200.0 mg Microcrystalline cellulose 23.5 mg 43.5 mg Aqueous lactose 60.0 mg 70.0 mg Polyethylene bilo Ketone K30 12.5 mg 15.0 mg Sodium starch glycolate 12.5 mg 17.0 mg Magnesium stearate 1.5 mg 4.5 mg (core weight) 120.0 mg 350.0 mg Membrane coating: Hydroxypropyl methylcellulose 3.5 mg 7.0 mg Polyethylene glycol 6000 0.8 mg 1.6 mg talc 1.3 mg 2.6 mg iron oxide (yellow) 0.8 mg 1.6 mg titanium dioxide 0.8 mg 1.6 mg 121967.doc -178- 200811112 The active compound is mixed into two # Q t β甲和/, microcrystalline cellulose, And the mixture is condensed into two::, a solution in water - granulation. The granules are mixed with the acid sulphate and the hard acid acid and (4) to produce 12 〇 hearts: 22: nucleus. The core was painted with the film coating aqueous solution/suspension fluid mentioned above. EXAMPLES Capsules containing the following ingredients can be made in a conventional manner: 25.0 nig per capsule 150.0 nig 20.0 mg 5.0 mg Ingredient Compound of formula (I) Lactose Corn starch Talc

The components are sieved and mixed and filled in capsule No. 2 Example C The injection solution may have the following composition: Formula (I) Polyethylene glycol 400 3·0 mg Acetic acid 150·° m8 Injection solution is transferred to pH 5.0 with water Make up 1.0 ml Dissolve the active ingredient in a mixture of polyethylene glycol 400 and a mixture of water (partial). The pH was adjusted to 5. 由 from acetic acid.蕤± Add the residual amount of water to the field to adjust the volume to 1 · 〇 ml. The solution was filtered and sterilized in a vial (using a suitable cover) and sterilized.

Example D Soft gelatin capsules containing the following ingredients can be made by customary formula. 121967.doc •179- 200811112 Capsule content Formula (1) Compound 5.0 mg Yellow wax 8.0 mg Hydrogenated soybean oil 8.0 mg Partially hydrogenated vegetable oil 34.0 mg Soybean oil 110.0 mg Capsule content weight 165.0 mg Gelatin capsule gelatin 75.0 mg Glycerin 85% 32.0 mg Karion 83 8·0 mg (dry matter) Titanium dioxide 0.4 mg Yellow iron oxide 1.1 mg The active ingredient is dissolved in the warm melt of the other ingredients and the mixture Fill in a suitable type of soft gelatin capsule. The filled soft gelatin capsules are processed according to the usual procedure. Example E A sachet containing the following ingredients can be made in a conventional manner: Compound of formula (I) 50.0 mg Fine powdered chyle 1015.0 mg Microcrystalline cellulose (AVICEL PH 102) 1400.0 mg Sodium carboxymethylcellulose 14.0 mg Polyvinylpyrrole Pyridone K 30 10.0 mg Magnesium stearate 10.0 mg Flavoring additive 1.0 mg The active ingredient is mixed with lactose, microcrystalline cellulose and sodium carboxymethylcellulose and granulated with a mixture of polyvinylpyrrolidone in water. The granules are mixed with magnesium stearate and a flavoring additive and filled in a sachet. 121967.doc -180-

Claims (1)

200811112 X. Patent application scope: 1. A compound of formula (I) R wherein R1 is €1, alkyl, lower alkoxy-lower alkyl, lower alkoxy-fluorenyl-lower alkyl, cycloalkyl, cycloalkyl-lower alkyl, aryl , aryl-lower alkyl 'di-aryl-lower alkyl, heteroaryl, heteroaryl-lower alkyl, heterocyclyl or heterocyclyl-lower alkyl, wherein cycloalkyl, The aryl, heteroaryl or heterocyclic group is optionally substituted by 1 to 3 substituents independently selected from the group consisting of: a lower carbon group, a lower alkoxy group, a lower alkoxy group - Alkyl, morphinyl, methionine, a hydroxy, a fluoro-lower alkyl, a fluoro-lower alkoxy, a lower alkyl carbonyl-hydrazine (lower alkyl), a lower alkane -carbonyl-oxime (Η), ΝΗ2, Ν (Η, lower alkyl), Ν (lower alkyl) 2, carboxyl, amide, hydrazine (hydrazine, lower alkyl) C(O) And N(lower alkyl) 2C(0); R2 is hydrogen or lower alkyl; R3 is lower alkyl, cycloalkyl, partially unsaturated cycloalkyl, aryl, aryl-lower alkyl , heteroaryl, heteroaryl-lower alkyl, heterocyclyl or heterocyclyl-lower alkyl, 121967. Doc - 1 - 200811112 wherein an aryl, heteroaryl or heterocyclic group is optionally substituted by 1 to 3 substituents independently selected from the group consisting of i, lower alkyl, lower alkane Oxy, lower alkoxy-carbonyl, hydroxy, fluoro-lower alkyl, fluoro-lower alkoxy, NH2, N(H, lower alkyl), N (lower alkyl) 2, low Carboalkyl-carbonyl-N (lower alkyl), lower alkyl-carbonyl-N(H), carboxyl, aminemethanyl, N(H, lower alkyl) C(0) and N (low Carboxyalkyl) 2C(0); R4 is a) heteroaryl optionally substituted with 1 to 3 substituents independently selected from the group consisting of lower alkyl, phenyl, lower alkane Oxy-carbonyl, carboxyl, aminecarbamyl, N(H, lower alkyl) C(O), N(lower alkyl) 2C(0), NH2, N(H, lower alkyl), N (lower alkyl) 2, lower alkyl-carbonyl-N (lower alkyl), lower alkyl carbonyl-N(H), hydroxy, lower alkoxy, halogen, fluoro-low carbon An alkyl group, a fluorine-lower alkoxy group, a cyano group and a morpholinyl group; b) an unsubstituted naphthyl group or one to three independently selected from the group consisting of the following groups Substituted substituted naphthyl or phenyl: A, hydroxy, NH2, CN, hydroxy-lower alkyl, lower alkoxy, lower alkylcarbonyl, lower alkyl-carbonyl-N(H), Lower alkoxy-carbonyl, amine-based, di-low-carbo-amine, carbaryl, fluorenyl, thienyl, pyrazolyl, oxadiazolyl, imidazolyl, triazole , tetrazolyl, 2-oxo-pyrrolidinyl, pyrrolyl, pyridyl, sigma-based, 2-sided oxy-bucking base, ° ratio, bite group, brigone, oxazolyl , thiazolyl, oxadiazolyl, carboxyl, lower alkane 121967. Doc -2- 200811112 base, fluorine-low carbon alkyl, fluorine-low carbon alkoxy, n (h, low carbon alkyl), N (low carbon alkyl) 2, lower alkyl carbonyl _N ( Lower alkyl), amine methyl sulfhydryl, N (H, low carbon alkyl) c (〇), n (low carbon alkyl) 2C (0), low hindrance - amine thiol, low carbon a phenyl group, a benzhydryl group, a phenoxy group, and optionally a phenyl group substituted with one or three substituents independently selected from a halogen and a fluorine-lower alkyl group; or c) if R3 is a cycloalkyl group, R4 R4 is also a phenyl group; R5, R6, R7 and R8 are each independently fluorene, arginine or lower alkyl, or R5 and R6 are bonded together, or r6&amp;R7 are bonded together. , or R7 and R8 are taken together, together with the carbon atom to which they are attached, form a 4-7 membered aromatic or non-aromatic carbocyclic or heterocyclic ring; and pharmaceutically acceptable salts and esters thereof; The condition is that the compound of the formula (I) is not selected from the group consisting of 2-[2-(2-gas-phenyl)-benzimidazole _ 丨-yl]_4-methyl-pentanoic acid butyl hydrazine. Amine and 2 dimethyl 2-benzo[丨,3]dioxol-5-yl-benzimidazol-1-yl)-N-benzylidene Guanamine. 2. The compound of claim 1, wherein R4 is a) optionally substituted by 1 to 3 heteroaryl groups selected from the group consisting of the following groups: lower alkyl, phenyl, low Carboalkoxy-carbonyl, carbyl, carbamoyl, N(H, lower alkyl) c(〇), N(lower alkyl) 2C(0), NH2, N(H, lower alkane Base), n (lower alkyl group) 2, lower carbon alkyl group - alkyl-N (lower alkyl group), lower alkyl group carbonyl group _N (H), hydroxyl group, 121967. Doc 200811112 low carbon alkoxy, _, fluorocarbon, and fluoro-low carbon sulphonate; b) unsubstituted naphthyl or 1 to 3 independently selected from the group consisting of Substituted substituted naphthyl or phenyl: halogen, hydroxy, NH2, CN, hydroxy-lower alkyl, lower alkoxy, lower alkyl-lower, low deflagration, Wei-N (H ), low carbon calcined base - Wei, alkyl aryl, di-lower alkyl-amine sulfonyl, lower alkyl-sulfonyl, thienyl, alpha ratio σ, σ sigma Sitting base, σ米ϋ sitting base, three σ sitting base, four xj sitting base, 2_ side oxy-17 pyrrole sigma, σ 洛洛基, 吼σ定基, mouth σ定基, 2-sided oxy-Brigade σ定基, σ比洛基基, 唆基基, 嗤 嗤, 嗟嗤, chelate, thiol, carbyl, fluoro-low carbon, fluoro-low carbon alkoxy, Ν (Η, lower alkyl), Ν (lower alkyl) 2, lower alkyl-carbonyl _ 低 (lower alkyl), amine methyl sulfonyl, hydrazine (hydrazine, lower alkyl) C ( O), hydrazine (low-stone anti-calcining) 2C (0) and low-carbon alkyl-amine thiol; or C) if R3 is a cycloalkyl, then R4 is a cycloalkyl group, and R4 may also be Phenyl. 3. The compound of claim 1 or 2, wherein R1 is Ciw alkyl, lower alkoxy-lower alkyl, lower alkoxy-carbonyl-lower alkyl, cycloalkyl, cycloalkyl Carboalkyl, phenyl, phenyl-lower alkyl, bis-phenyl-lower alkyl, heterocyclic or heterocyclic-lower alkyl, wherein the heterocyclic group is selected from piperidinyl and 2 a group of pendant oxy-pyrrolidinyl groups wherein cycloalkyl, phenyl or heterocyclic groups are optionally substituted by 1 to 3 substituents independently selected from the group consisting of: lower alkyl , low % I alkoxy, lower alkoxy carbonyl, morphinyl and formamidine. 4. The compound of claim 1 or 2, wherein 1 is (: 11 () alkyl, cycloalkyl or phenyl' wherein the phenyl group is optionally independently selected from the group consisting of lower alkyl groups 121967. Replacement of the substituent of doc 200811112. 5. A compound according to claim 1 or 2, wherein R1 is hydrazine, [,3,3-tetramethyl-butyl, cyclopentyl, cyclohexyl or 2,5-dimethyl-phenyl. 6. A compound according to claim 1 or 2, wherein R1 is tetrahydropyranyl, a cycloalkyl group substituted by is 2 im groups or a phenyl group substituted by 1 to 2 lower alkyl groups. 7. The compound of claim 6, wherein R1 is tetrahydropyran-4-yl, 4,4-di-2-carbonate or 2,6-dimercapto-phenyl. 8. A compound according to claim 1 or 2, wherein r2 is hydrogen. 9. The compound of claim 1 or 2, wherein R3 is lower alkyl, cycloalkyl, partially unsaturated cycloalkyl, phenyl, phenyl-lower alkyl or heteroaryl, wherein the hydroxy group is The group consisting of a quinone group and a benzodioxolyl group is selected, wherein the phenyl group or the heteroaryl group is optionally substituted with 1 to 3 substituents independently selected from the group consisting of: Element, lower alkyl, low carbon alkoxy, hydrazine 2, hydrazine (hydrazine, low carbon alkyl) and hydrazine (low carbon alkyl) 2. 10. A compound according to claim 1 or 2, wherein R3 is cycloalkyl, phenyl, phenyl-lower alkyl or a carbyl group. 11. The compound of claim 1 or 2, wherein R3 is cyclopentyl, cyclohexyl, phenyl, 3-phenyl-propyl or σ-pred-2-yl. 12. A compound according to claim 1 or 2, wherein R3 is lower alkyl, tetrahydropyranyl or substituted by 1 to 3 substituents independently selected from fluoro-lower alkyl and fluoro-lower alkoxy Phenyl. A compound according to claim 9, wherein R3 is isobutyl, pentyl or tetrahydropentan-2-yl. 121967. Doc 200811112 14 · A compound according to claim 1 or 2, wherein r4 is a) a heteroaryl group selected from the group consisting of thienyl, pyrrolyl, 2-formoxy-1,2-dihydro- Pyridinyl, fluorenyl, quinalyl and anthracene, 3_one oxy-isoindenyl'. The heteroaryl group is optionally selected from the group consisting of a lower alkyl group and a phenyl group by 1 to 2 a substituent substituted; b) an unsubstituted naphthyl group or a naphthyl group or a phenyl group, which is substituted with a substituent independently selected from the group consisting of: hydroxy, NH2, CN,没-low-carbon alkyl, low-carbon alkoxy, low-carbon alkyl-Weiyl, lower alkyl-carbonyl-N(H), lower alkoxy-carbonyl, aminesulfonyl, di-low Carboalkyl-amine fluorenyl, low carbon alkyl-continuary thiol, thienyl, pyrazolyl, thiadiazolyl, imidazolyl, triazolyl, tetrazolyl, 2-tertyloxy-bromolidinyl Or C) If R3 is a cycloalkyl group, R4 is a cycloalkyl group, and R4 may also be a phenyl group. 15.  A compound according to claim 2 or 2, wherein r/ is a) a heteroaryl group selected from the group consisting of thienyl, 2 • pendant oxy-1,2-dihydro-pyridyl and quinolyl Wherein the thienyl group is optionally substituted by a phenyl group; or b) an unsubstituted naphthyl group or a phenyl group via a base substituted with 1 to 2 substituents independently selected from the group consisting of: Base, low carbon alkoxy, lower alkyl-carbonyl-N(H), imidazolyl or tetrazolyl. 16.  A compound of the invention, wherein R4 is 2,4-dimethoxy-phenyl, 2, 4-methylmethyl-phenyl, 4-(tetrampan-5-yl)phenyl, 4 -(Husin-2-yl)-phenyl, erythridinyl-phenyl, 5-phenyl-porphin 121967. Doc 200811112 base, 2-sided oxy-hydrazine, dihydro-hydrazine|yl or porphyrin winter base. 17. A compound according to claim 1 or 2, wherein ... is a) a heteroaryl group selected from the group consisting of pyridyl, pyrazolyl, isoxazolyl, benzimidazolyl, furyl, thiophene a base, a fluorenyl group, a benzo[b]thienyl group, a benzothiazolyl group, a benzofuranyl group, and a quinoxalinyl group, the heteroaryl group being optionally selected from the group consisting of 1 to 2 independently Group substituent substitution: halogen, CN, NH2, N (lower alkyl) 2, lower alkyl, lower alkoxy, fluoro-lower alkyl and morpholinyl; or b) unsubstituted Naphthyl or a naphthyl or phenyl group substituted with 1 to 3 substituents independently selected from the group consisting of: an amine methyl group, a halogen, a lower alkyl group, a fluorine-lower alkyl group, a fluorine group Lower alkoxy, lower alkenyl, N (lower alkyl h, n(H, lower alkyl) CO, benzamidine, phenoxy and optionally 1 to 3 independently selected from a phenyl group substituted with a substituent of a fluorine-lower alkyl group. 18. A compound according to claim 17, wherein the thiophene group substituted by a sulphate; or b) a benzene substituted with an amine carbaryl group or a halogen base. 19. The compound of claim 18, wherein R4 is 5-chloro-thiophen-2-yl, 2-aminocarbonyl-phenyl or 4-chloro-phenyl. The compound of claim 1 or 2, wherein R 5 , R 6 , R 7 and R 8 are each independently hydrazine, halogen, lower alkyl or lower alkoxy, or R 6 & R 7 are bonded together with The attached carbon atoms together form a 6-membered aromatic carbocyclic ring. 121967. Doc 200811112 21.  twenty two.  twenty three.  twenty four.  25.   A compound of claim 1 or 2 wherein R5 is hydrogen. A compound according to claim 1 or 2, wherein R6 is hydrogen, i or thiol. A compound of claim 1 or 2 wherein R7 is hydrogen, fluoro or chloro. A compound of claim 1 or 2 wherein R8 is hydrogen. The compound of claim 1 or 2, which is selected from the group consisting of 2,N-dicyclohexyl-2-(2-phenyl-benzimidazole-indole-ylacetamide hydrochloride, 2- [2-(4-Gas-phenyl)-benzopyrimidine 0-small base]_4_methyl-decanoic acid cyclohexyldecylamine, 4-{1 己-yl-(4-morpholinyl-phenylamine) Mercapto)_methyl]·1H_benzopyran-2-yl}-benzoic acid methyl ester hydrochloride, 2,N-dicyclohexyl-2_[5,6_digas·2_(2,4 -dimethoxy-phenylbenzimidazol-1-yl]-acetamide, 2-cyclohexyl-2-[2-(2,4-dimethoxy-phenyl)-benzene (tetra) oxime ]]_N_isopropyl-acetamide hydrochloride, 2, Ν·dicyclohexyl·2_[2_(4-methoxy-phenyl) benzoxanthene-1-yl]-acetamide hydrochloride Salt, 2, fluorene-dicyclohexyl·2·[2·(3·methoxy-phenyl&gt; stupid and azo. sitky base)_acetamide hydrochloride, 2, fluorene-dicyclohexyl- 2-[2_(2-methoxyphenyl)-benzopyrimidinyl]•acetamidine hydrochloride, 2, fluorene-dicyclohexyl-2-(2U•yl·benzo-salt ) · acetamidine hydrochloride, 2,N-dicyclohexylethoxyphenyl) _ 并 and Mi Mi Xiaoji] B 121967. Doc 200811112 guanamine hydrochloride, N-cyclohexyl-2 case 2, cardiomethoxyphenyl) benzophenanthine m] ice phenyl-butanamine, N_cyclohexyl-2-[2_(2 ,4-dimethoxy-phenyl)-benzo-flavor m]_3_methyl-butanamine hydrochloride, N-cyclohexyl-2-[2-(2,4-dimethoxy-phenyl) ) · stupid imidazole q•yl]^ phenyl-propanamide hydrochloride, N-cyclohexyl-2-[2-(2,4-dimethoxy-phenyl)-benzopyrene Keb 2_pyridin-2-yl-acetamide hydrochloride, N-cyclohexyl-2-cyclopentyl-2·[2_(2, cardiomethoxy-phenyl)-benzopyrene 1 -yl]-acetamide hydrochloride, 4-{1-[cyclohexyl-(cyclohexylaminecarbazyl-methyl)]_1Η_benzimidazolyl}-benzoic acid methyl ester, 2, fluorene-di Cyclohexyl-2-(2-naphthalen-2-yl-benzimidazol-1-yl)-acetamide, 2,N-dicyclohexyl-2-[2-(3-thienyl-phenyl)- Benzimidazole-:μpyridylamine, 2,yidihexyl-2-[2-(5-phenyl-thiophen-2-yl)-benzimidazole-indenyl]-acetamide, 3 -{1_[cyclohexyl-(cyclohexylaminemethylmercapto-fluorenyl-indolebenzimidazole_2-yl}-benzoic acid methylg, 2-[2-(3-hydroxy-phenyl-phenylene) Imidazole Bu 4_ methyl - cyclohexyl Amides acid, 2- [2- (4_M-phenyl) benzimidazole-_ _ small Jibu 4_ acid methyl cyclohexyl Amides, 121,967. Doc 200811112 2-[2·(1Η-σ引嗓-5-yl)-benzopyrene ϋ 基 4 4 - - - 4 4 4 4 4 4 , 2- 2- 2- 2- 2- 2- 2- 2- 2- 2- 2- 2- 2- 2- 2- 2- 2- 2- 2- 2- 2- 2- 2- Bowbuff-6-yl)-benzopyrimidine.坐小基卜4-甲| L soil J τ-kilopentanoic acid cyclohexyl decylamine, 2-[2-(4-amino-phenyl)-benzo-p-butyl hydrazine-ΐ-yl]-'-formamidine τ 暴 - Cyclohexyl decyl valerate, 2-cyclohexyl-2-[2-(2,4-dimethoxy-phenyl)-benzimidazole small quinone ((R)l-benzene -ethyl)-acetamide, 2,N-dicyclohexyl-2-[2-(4-hydroxymethyl-phenyl)-benzimidazole _ 丨-yl]- acetamidine, N·cyclo Hexyl-2-[2-(2,3-dimethoxy-phenyl)-benzimidazole _ 丨-yl group &gt; 4 phenyl-butanamine, 2- [2-(3-cyano-benzene) -benzimidazol-1-yl]-2,N-dicyclohexyl-acetamide, 2,N-dicyclohexyl-2-{2-[4-(1Η-tetrazol-5-yl) -phenyl]-benzimidazol-1-ylacetamide hydrochloride, 3-[1-(benzylaminocarbamoyl-cyclopentyl-methyl)_1H-benzimidazol-2-yl ]-N-benzoate benzoate, 2_[2-(2,4-cyclodecyloxyphenyl)-benzo[:7m嗤-1·yl]·hexanoic acid hexyl decylamine, 2,N-di Cyclohexyl-2-[2-(3-methanesulfonyl-phenyl)-benzimidazol-1-yl]-acetamide hydrochloride, N-benzyl-2-cyclohexyl-2-[ 2-(2,4-dimethoxy-phenyl)-benzimidazol-1-yl]-acetamide, 121967. Doc -10- 200811112 2-Cyclohexyl-2-[2-(2,4-dimethoxy-phenyl)-benzimidazole-p-(1-methylbutyl)-acetic acid amine, 4-[ 1-(phenylhydrazinocarbamyl-cyclopentyl-methyl | soil / benzimidazole_2·methyl benzoate, soil *^ N_cyclopentyl-2-[2-(3_曱 oxygen Phenyl))benzimidazole 丨 基 基 心 心 心 笨 笨 笨 笨 , , , , , , , ) ) ) ) ) ) ) [ [ [ [ [ [ [ [ [ [ [ [ [ [ [ [ 2-(2,4·imidazol-1-yl)-acetamide hydrochloride, 2-[2-(4-chloro-phenyl)-benzimidazole-bukib 2,N_: 衣χχ巷- Ethylamine hydrochloride, hydrazine-diphenylmethyl-2-cyclohexyl_2_[2_(2,4-dimethoxy. stupyl)- benzoimidazol-1-yl]-acetamide, hydrazine -Benzyl-2-(2-naphthalen-1-yl-benzimidazole-1.yl)_4_styl-butanamine, 2-cyclohexyl-2- [2-(2,4-dimethyl) Oxy-phenyl) _ 并 嗤 嗤 工 工 工 工 4- 4- 4- (4-methoxy phenyl)-acetamide, 2, N-dicyclohexyl-2-[2·(2,4-di曱oxy-phenyl)_4_methyl_benzoxazol-1-yl]-acetamide, 2, fluorene-dicyclohexyl-2-{2·[3-(2- oxo-oxime)洛定基)_phenyl]_benzimidazole-l-yl}-acetamide hydrochloride 2, Ν-dicyclohexyl·2-[2-(2· sideoxy-1,2-dihydrobiti-4-yl)-benzimidazol-1-yl]-acetamide, oxime-ring Pentyl-2-[2-(2-methoxy-phenyl)-benzoimylidene-1-yl]-4-phenyl-butanamine, 2-cyclohexyl-2-[2-(2 , 4-dimethoxy-phenyl)-benzopyrene-yl]_ν_ 121967. Doc -11 - 200811112 pentyl-acetamide, N-benzyl-2-(2-(4-chloro-phenyl)-benzimidazole 丨-yl]cyclopentamidine hydrochloride, 2,N-dicyclopentyl-2-(2-na-1-yl)bumimidazolylacetamide, 2-[2-(3-cyano-phenyl)-benzoxazole-I group ]_N_cyclohexylphenyl-butanamine, 2-[2-(4-carbyl-phenyl)-benzoimylidene-1_yl]_4_methylmethicin-decanoic acid cyclohexylamine Hydrochloride, N-t-butyl-2-cyclohexyl-2-[2-(2,4.dimethoxy-phenyl)- oxazol-1-yl]-acetamide, 4-[ W1-Benzylaminoindolyl-3-phenyl-propyl)-indoleimidazolyl]-benzoic acid methyl ester, _ 4-[1-(1-cyclohexylaminecarbamyl-3- Phenyl-propyl bromide and imidazole J-methyl]-benzoic acid methyl ester, 2,N-dicyclopentyl-2_[2-(2-methoxyphenyl)benzimidazole_i_ Bis-acetamide, 2,N-dicyclohexyl_2-[2-(2,4-dimethoxy-phenyl)-naphtho[2,3-d-bazozol-1-yl]-acetamidine Amine, 2-[2-(2,3-dimethoxy-phenyl)-benzimidazole-indenyl]methyl-pentanoic acid hexyl decylamine, < N-benzyl-2-[2- (2-methoxy-phenyl)_benzimidazole_1β-based]_4_benzidine Amine, &amp; 2- cyclohexyl-2- [2- (2,4-dimethoxy - phenyl-benzimidazole Ji Bu n (3- isopropoxy-propyl) - _ as acetamide, 121,967. Doc -12- 200811112 2-[2-(2,4-dimethoxy-phenyl)·benzimid-1-yl 1 1 1 iso-indolyl, 4 phenyl-butanamine, _ N- Benzyl-2-cyclopentyl-2-(2-naphthalen-1-yl-benzomidine. sitting ^ ''base) · ethylamine, S 2,N-dicyclohexyl-2-[2- (2,3-Dimethoxy-phenyl)-benzimidazoleacetamidamine, _yl]-2-[2-(2,4-methoxycarbonyl-benzyl)-benzophenanthrene. Sitting -1_base 1_4 trial τ volume - valeric acid cyclohexyl decylamine, 2-cyclohexyl-2-[2-(2,3-dimethoxy-phenyl)-benzimidazolyl]_N_isopropyl Ethylamine, 2-[2-(2,3-dimethoxy-phenyl)-benzimidazole _ 丨-yl]-N-isopropyl_4_phenyl-butanamine, 2-[ 2-(4-Ethyl-phenyl)-benzimidazolyl]-N-cyclohexylphenyl-butanamine, N-benzyl-2-[2-(4-chlorophenyl) Olefinic acid group]_4·phenylbutylideamine hydrochloride, 4-[1-(1-isopropylaminocarbazinyl-pentyl) benzo oxime | benzyl] methyl benzoate, N-butyl -2-[2-(2,4-dihydrogen, its lean |, μ, thiol-bens)-benzimidazole-^ phenyl phenyl-acetamide, 2-[2-(2 , 3 —Methyl propyl phenyl” benzophenanyl] winter methyl isopropyl decyl amide, 2 - benzoquinone [1,3] dioxagen, 隹, 隹Alkene-5-yl-indole-butyl·2-[2-(2,3-dimethoxy-phenyl)·benzo(tetra)]-yl]-ethylamine, 121967. Doc -13- 200811112 2-Benzo[1,3]dioxole_5•yl_N•butyl·2_[2_(2*-oxy-phenyl)-benzimidazole-1 -yl]-acetamide, formazan-butyl-2·[2-(2,4-dimethoxy-phenyl)-benzoic acid-small-small-gas-phenyl)-ethylamine Ν-cyclopentyl-2-|&gt;(3-carbyl-phenyl)-benzopyranyl hydrazine _ bromoamide, turd 2-[2-(4-ethyl fluorenyl-phenyl) )_Benzene-small-small base]_isopropyl hexanoate &amp; υ[[2·(2,3-dimethoxy-phenyl)·benzo-flavor^ = keto-amine, soil]-2 -本2-[2-(4-Ethyl-phenyl)-benzimidazole-diyl] decylamine, methyl-decanoic acid cyclohexanyl-butyl-2-[2-(2,3 _Dimethoxy. Phenyl)-benzopyrene-t-tolyl-acetamide, hydrazine-butyl-2-[2-(2,3-dimethoxy-phenyl)-benzimidazole methoxy-benzene Ethylamine, Ν-butyl-2-|&gt;(2,3-dimethoxyphenyl&gt; stupid and imidazolyl), gas-based, ethylamine, hydrazine Base_2_|&gt;(2,3-dimethoxyphenyl)_ is stupid. Mazole+yl]·dimethylamino-phenyl)-acetamide, 2-[2-(2,3-dimethoxy-phenyl)-benzopyrene + isopropyl bromide Alkylamine, 4-{1·[(2-fluoro-phenyl)-isopropylaminecarbazyl-methyl]_ih_ benzoimidazole-methyl-2-brombenzoate, ' _ cyano- Phenyl)-benzo benzoyl-methyl-decanoic acid cyclohexyl 121967. Doc •14- 200811112 Indoleamine, 2-[2-(3-Gas-phenyl)-benzo-flavor m]-4-methyl-decanoic acid cyclohexylamine, N-butyl-2-[2- (2,4-dimethoxy-phenyl)-benzamidazolyl]_2-(4-methoxy-phenyl)-acetamide, N-benzyl-2-[2-(3- Oxy-phenyl)-benzimidazolyl]_4_phenyl-butanamine hydrochloride, 2-(4-chloro-phenyl)-2-[2-(2,3-dimethoxy- Phenyl)-benzimidazole-bukib N-isopropyl-ethylamine, N-butyl-2_[2-(2,4-methoxy-phenyl)-benzoiminyl ]_2_(4-dimethylamino-phenyl)-acetamide, 2-[2-(4-hydroxy-phenyl)-benzimidazole isopropyl-4-phenyl-butanamine, 2- [2-(4-Hydroxy-phenyl)-benzimidazole-fluorenyl]-'methyl-pentanoic acid cyclohexyl decylamine, 2-[2-(3-a-phenyl)-benzimidazole _ ;^基]_N_isopropyl_4_phenyl·butanamine, N-butyl-2-(4-chloro-phenyldimethoxy-phenyl)-benzimidazol-1-yl] - acetamide, 2-[2-(3-cyano-phenyl)-benzimidazole _ 丨 _ _ _ _ _ _ _ _ _ phenyl phenyl Ethyl phenyl-phenyl benzoimidazole _ 丨-yl]_N_isopropyl 2 4 4 methoxy-phenyl) Stuffed amine, 1_ {4- [isopropyl-carbamoyl acyl _ methoxy - phenyl) _ methyl] _1H_ benzo 121,967. Doc -15- 200811112 imidazol-2-yl}-benzoic acid methyl _, 4 - [ 1 -(isopropylamine guanidine turtle f V dumb cuminyl-methyl)-1 Η-benzimidazole-2- Methyl benzoate, N-isopropyl-2-[2-(1_methyl-T-yl-1H-pyrrole-2-yl)·benzimidazole-^yl-4-phenyl-butane Amine, 2-[2-(3-cyano-benyl)-benzimidazole]• isopropylguanidinium amide, 2·[2_(4-hydroxybenzyl)-benzimidazole Isopropyl decylamine, 2-benzopyrene '3]dioxol-5_yl_n_butyl·2·[2_(bumethyl-1 Η-pyrrole-2-yl)-benzimidazole Ethylamine, 2-cyclohexyl-2-[2-(2,4-didecyloxy-phenyl)-benzo[indolyl]-[2,6-dimethyl-benzene Ethylamine, 2,N-dicyclohexyl-2_[2_(2,4.dimethoxy-phenyl)-benzo(tetra))-acetic acid amine, 2_cyclohex-3-ene Base-oxime-cyclohexyl_2_[2_(2,4-di-foxy-phenyl)-benzimidazol-1-yl]-acetamide, 2-called 4-cyano-phenyl)-benzene And miso Xiaoji]_2# Dicyclohexyl_Ethylamine hydrochloride, 2: Hexyl-N-cyclopentyl-2, 4_Dimethoxy-phenyl)_Benzene saliva·1 - Base l·acetamide, 2, Ν·二环己_2, 4,4-dimethoxy-phenyl) from diimidazol-1-yl]-acetamide, 2, Ν·dicyclohexyl·2_[2_(2,4_:methoxy). ]-Acetamine, , basic open pearl print - (4, chloro-phenyl) · benzopyrene · i • base] 2, ν_ dicyclohexyl broth 121967. Doc -16- 200811112 Amine, 2,N-dicyclohexyl-2-[2-(4-aminosulfonyl-phenyl)-benzimidazole _ 丨-yl]- acetamidine hydrochloride, 2- Cyclohexyl-2-[2-(2,4-dimethoxy-phenyl)-benzopyranyl]_n_(1,1,3,3-tetramethyl-butyl)-ethonamide , 4-{[1-cyclopentyl-(cyclopentylaminemethanyl-methyl)]_1H-benzimidazole_2-yl}-benzoic acid methyl ester hydrochloride, 2,N-dicyclohexyl- 2-(2-quinoline-6-yl-benzimidazolyl)-acetamide hydrochloride, 2-[2-(4-aminophenyl)-benzimidazole·丨-kib Dicyclohexyl-acetamide, 2-[2-(2,4-dimethoxy-phenyl)-benzimidazole _ 丨 _ _ _ 5 phenyl pentanoic acid cyclohexyl decylamine hydrochloride, 4-[1-(1-cyclopentylaminecarbazinyl-3-phenyl-propyl)_1H-benzimidazole_2-yl]-benzoic acid methyl ester, 2,N-dicyclohexyl-2_[2 -(4-didecylamine sulfonyl-phenyl)-benzimidazole _ 1_yl]-acetamide hydrochloride, 2,N-cyclohexyl-2-[2-(3-amine) _-phenyl)_benzoimylidene-1-yl]-acetamide hydrochloride, 2,N-dicyclohexyl-2-{2-[&gt;(1Η-tetrazole_5_yl) Phenyl]-benzimidazole·1-yl}-ethylamine hydrochloride , 2,N-dicyclohexyl-2-{2-[4-(1Η-imidazol-2-yl)-phenyl]-benzimidazole-1-yl}-acetamide hydrochloride, 2, Dicyclohexyl-2-[2-(4-imidazolyl-1-yl-phenyl)-benzimidazole-1-yl].   •17- 121967. Doc 200811112 acetamide hydrochloride, 2,N-dicyclohexyl 2 -[2-(4-[1,2,4]triazol-4-yl-phenyl)-benzimidazole _ 1 -yl ]-acetamide hydrochloride, 2,N-dicyclohexyl_2-{2_[4_(1Η-oxazol-4-yl)-phenyl]-benzimidazole _ 1 -yl}-acetamide Hydrochloride, 2,N-dicyclohexyl-2-[2-(4-[1,2,3]thiadiazol-4-yl-phenylbenzomidine-1-yl]-ethyl Amine hydrochloride, 2,N-dicyclohexyl-2-[2-(1,3-di-dioxy-2,3-dihydro)H-isoindole-5-yl)-benzopyrimin -1-yl]-acetamide hydrochloride, 2,N-dicyclohexyl-2-[2-(3-tetrazole-fluorenyl-phenyl)benzoimidazole 丨 基 基 基Amine hydrochloride, 4-[1-(cyclohexyl-3-decyloxycarbonylphenylamine fluorenyl-methyl)_1H-benzoimin-2-yl]-benzoic acid methyl ester hydrochloride, 4-(1-{cyclohexyl-[(4-methoxycarbonyl-cyclohexylmethyl)-amine-carbamoyl]-methyl}-1Η-benzoimidazol-2-yl)-benzoic acid decyl ester Hydrochloride, 4-{2-cyclohexyl-2-[2·(4-methoxycarbonyl-phenyl)-benzimidazole 丨-yl]- ethionylpiperidine-1 -carboxylic acid Ethyl ester hydrochloride, Ν-cyclohexyl-2-[2-(2,4-dimethoxy-phenyl)-benzene Imidazole βΐ_yl]_2_phenyl-acetamidine hydrochloride, 4-(1-{cyclohexyl-[3-(2-oxo-oxypyrrolidine)-propylamine-methyl)-- Methyl}-1Η-benzimidazole_2-yl)-benzoic acid methyl ester hydrochloride, 4-{1-[cyclohexyl-(3-methoxycarbonyl-propylaminecarbamyl)-methyl] _ιη_ Benzomidino-2-yl}-benzoic acid methyl ester hydrochloride, 4-{1-[cyclohexyl-(4-methoxycarbonyl·butylaminecarbamyl)&gt;methyl]^η_ 121967 . Doc •18· 200811112 Benzomidazole _ q , μ -2-yl}_benzate carboxylic acid ester hydrochloride, hexyl-(5-methoxyl-ylpentylamine-methyl)-methyl].   本开咪呼〇#扣& ” to methyl benzoic acid methyl ester hydrochloride, 2-cyclohexylamino 2-[2_(2,4-dimethoxy-phenyl)-benzoic Rice saponin]_ν_ Τ hexylamine hydrochloride, 2-"2-(4_7-S-Slanylamino-phenyl)-benzimidazole-i_基卜2 Ν二产基-乙醯, , , , , , , , , , , , , , , , , , , , , , , , , , , , , , , , , , , , , , , , , , , , , , , , , , , , , , , , , , , , , 1 [飧-hexyl-(3-carbamidophenylamine-methyl fluorenyl)-methyl b 1 benzobenzyl-2-ylpyridinic acid methyl ester hydrochloride, and clothing, base-2- (2_naphthalen-1-ylbenzimidazolyl)-propionamide, and its pharmaceutically acceptable salts and esters.   A compound of claim 1 or 2, which is selected from the group consisting of N-hexylyl_2_[2_(2,4-dimethoxy-phenyl)_benzimidazole_ι_yl]_2_比 pyridine-2-yl-acetamide hydrochloride, Ν-cyclohexyl-2-cyclopentyl 2 -[2-(2,4-dimethoxy-phenyl)-benzopyrene _ 1-yl]-acetamide hydrochloride, 2, fluorene-dicyclohexyl-2-(2-naphthalen-2-yl-benzimidazol-1-yl) acetamidine, 2,N-bicyclic Hexyl-2-[2_(5-phenyl-thiophen-2-yl)-benzoimidazolium-fluorenyl]-ethylamine, 2,N-dicyclohexyl-2·[2-(4-hydroxyl) Benzyl-phenyl)-benzimidazole-diyl]-acetamide, 121967. Doc -19- 200811112 2, Icyl-Hexyl 2,2-{2_[4_(1H_tetrazol-5-yl)-phenyl]-benzimidazole-1 1-yl}-Ethylamine hydrochloride, 2 , N-dicyclohexyl m-(2,4-dioxaoxy-phenylindolyl-benzo-yt-yl-1-yl]-ethanoamine hydrochloride, 2,N-dicyclohexyl_2 -[2-(2-Sideoxy 4,2-dihydro-pyridine-4-yl)-benzimidazol-1-yl]-acetamide, 2-cyclohexyl-2-[2-(2, 4_didecyloxy-phenyl)_benzimidazole_丨_yl]_n_(2,6-dimethyl-phenyl)-acetamide, 2-cyclohexyl-N-cyclopentyl_2_[ 2_(2,4-dimethoxy-phenyl)_stupid and salivary _ 1-yl]-acetamide, 2-cyclohexyl-2-[2-(2,4-dimethoxy-benzene ())benzimidazole-based (1,1,3,3-tetradecyl-butyl;)_acetamide, LN-cyclohexyl-2·(2_啥琳冬基_Benzene And imidazole + yl) acetamidine hydrochloride, 2-[2_(2,4-dimethoxy-phenylbenzimidazolyl)-5-phenyl-pentanoic acid cyclohexyl decylamine hydrochloride, 2, Ν-Dicyclohexyl-2-{2-[4_(1Η·imidazol-2-yl)phenyl]-benzimidazole-1-yl}-acetamide hydrochloride, Ν-cyclohexyl-2- [2-(2,4-dimethoxy-phenyl] cum-imidazole-bubub^phenyl-acetamide salt Acid salt, and 2-[2-(4-acetamidoamino-phenyl)-benzimidazole _i-yl]-2, fluorene-dicyclohexyl-acetamide, and pharmaceutically acceptable thereof Salts and esters. 27. The compound of claim 1 or 2, which is selected from the group consisting of: 121967. Doc • 20 - 200811112 2,N - diatom hexyl-2 - (2-phenyl-benzoquinone σ-l-yl)-ethonamide '2-[1-(cyclohexyl-cyclohexylamine) Base-mercapto)-1Η-benzoimidazol-2-yl]-benzamide, 2-[2-(5-amino-penridin-2-yl)-benzimidazole-1-yl]- 2,&gt;^dicyclohexyl-acetamide, 2, fluorene-dicyclohexyl-2-[2-(2-ethyl-5-methyl-211-pyrazol-3-yl)-benzimidazole -1_基]-acetamidamine, 2,^^di-dihexyl-2-[2-(5-methyl·iso-°°°_4_yl)_benzoquinone-salt-1_yl]-B Amine amine ' 2,yicyclohexyl-2-[2-(111-fluoren-2-yl)-benzimidazol-1-yl]-acetamide, 2-(1Ή-[2,5'] Bibenzimidazol-1-yl)-2, fluorene-dicyclohexyl-acetamide, 2, fluorene-dicyclohexyl-2-(2-furan-2-yl-benzimidazole-1-yl)- Acetamine, 2-[6-bromo-2-(4-chloro-phenyl)-benzimidazol-1-yl]_2,&gt;^dicyclohexyl-acetamide, 2-[6-gas- 2-(4-Chloro-phenyl)-benzimidazole-1-yl]-2,N-dicyclohexyl-acetamide, 2-[2-(4-chloro-phenyl)-6-methoxy -benzimidazol-1-yl]-2,N-dicyclohexyl-acetamide, 2-[6-Gas-2-(4-chloro-phenyl)-5-fluoro-benzimidazole-1 -yl]-2,N-dicyclohexyl-ethinamine '(S)-2,N-dicyclohexyl-2-[2-(2,4-dimethoxy-phenyl)·benzimidazole -1-yl]-acetamide, (S)-2-[2-(4-chloro-phenyl)-benzimidazol-1-yl]-2,N-dicyclohexyl-ethene-121967. Doc -21 - 200811112 Amine, 2-[ 1-(cyclohexyl-cyclohexylaminecarbazyl-methyl)-1H-benzoimidazol-2-yl]-N-methyl-benzamide, 2 Ν-. ^D-Hexyl-2-(2-Fufuran-3-yl-benzoquinone 1:7 m唆-1 -yl)-Ethylamine ' 2,Ν-Dicyclohexyl-2-[2-(3- Mercapto-furan-2-yl)-benzimidazol-1-yl]-acetamide, 2, fluorene-dicyclohexyl-2-[2-(3-methyl-isoxazol-5-yl) -benzimidazol-1-yl]-acetamidamine, 2, fluorene-dioxime-yl-2-(2-m-tolyl-benzoquinone-l-yl-yl)-ethonamine 2,N - Dioxahexyl-2-[2-(3-^-phenyl)-benzoic. Sodium-1-yl]-ethylamine, 2,N-dioxadecyl-2·[2-(2-Gas-phenyl)-benzomime-1-yl]-ethanoamine, 2, Ν - 二 哀 己 - - 2- [2-(3,5-didecyl-iso 0 ° ° 圭-4-yl)-benzoquinone miso-1-yl]-acetamide, 2, Ν- 2-[2-(3-fluorenyl-σ-sec-2-yl)-benzoquinone miso-1-1-yl]-acetamide, 2, fluorene-dicyclohexyl-2- [2-(4-vinyl-phenyl)-benzimidazol-1-yl]-acetamide, 2,N-dicyclohexyl-2-[2-(2,3-dimethyl-phenyl) )-benzimidazole·1_yl]-ethanoamine, 2, fluorene-dicyclohexyl-2-[2-(3,4-dimethyl-phenyl)-benzimidazol-1-yl]- Acetamine, 2,N-dicyclohexyl-2-[2-(4-ethyl-phenyl)-benzimidazol-1-yl]-acetamidine 121967. Doc -22- 200811112 Amine, 2, Ν-, a cumyl- 2- [2-(2,4-dimethyl-phenyl)-stupid and 117 m sigma-1 -yl]-acetamide, 2, Ν-二 哀 己 · · · 2-[2-(2-ethyl-phenyl)-benzoquinone 11 m sate-1 · yl]-ethylamine, 2, fluorene-dicyclohexyl-2-[ 2-(4-Fluoro-3-indolyl-phenyl)-benzimidazol-1-yl]-acetic acid amine, 2, Ν·dicyclohexyl-2-[2-(3-fluoro-4-methyl) -Phenyl)-benzimidazol-1-yl]-ethonamide, 2, fluorene-di- hexyl- 2-[2-(2,6-di-phenyl-phenyl)-benzoquinone 17 m°- 1 -yl]-ethanoamine, 2, fluorene-dicyclohexyl-2-[2-(3,5-difluoro-phenyl)-benzimidazol-1-yl]-acetamide, 2, hydrazine -dicyclohexyl-2-[2-(2,5-difluoro-phenyl)-benzimidazol-1-yl]-acetamide, 2, fluorene-dicyclohexyl-2-[2-(3 ,4-difluoro-phenyl)-benzimidazole-1-yl]-acetamide, 2, fluorene-dicyclohexyl-2-[2-(2,3-difluoro-phenyl)-benzo Imidazolyl-1-yl]-acetamide, 2, fluorene-dicyclohexyl-2-[2_(1Η-吲哚-4.yl)-benzimidazol-1-yl]-acetamide, 2, hydrazine -dicyclohexyl-2-[2-(1Η-indol-6-yl)-benzimidazol-1-yl]-acetamidamine, 2-[2-(5-chloro-thiophen-2-yl) -Benzene 1-yl] -2, Ν- dicyclohexyl - B 121 967. Doc -23- 200811112 decylamine, 2-[2-(4-acetamido-phenyl)-benzimidazol-1-yl]-2,N-dicyclohexyl-acetic acid amine, 2-[2-( 2-Ethyl-phenyl)-benzimidazole-1.yl]-2,N-dicyclohexyl-acetic acid amine, 2,N-dicyclohexyl-2-[2-(4-isopropyl- Phenyl)-benzimidazol-1-yl]-acetic acid amine, 2-[2-(4-carbyl-2-cyclo-phenyl)-benzoquinone. -1--1-yl]-2,N-dicyclohexyl_acetamide, 2,N-di-f-hexyl-2-[2-(2-dimethylamino)phenyl)-benzoquinone 1^ 0 sit-1_yl]-acetamide, 2,N-dicyclohexyl-2-[2-(3-dimethylamino-phenyl)-benzimidazol-1-yl]-acetamide, 2,N-Dicyclohexyl-2-[2-(4-methoxy-3-(indolyl-phenyl)-benzimidazole-1-yl]-acetamide, 2,N-dicyclohexyl- 2-[2-(4-Methoxy-2-methyl-phenyl)-benzimidazol-1-yl]-acetamide, 2,N-dicyclohexyl-2-[2-(3- Methoxy-4-methyl-phenyl)-benzimidazol-1-yl]-acetamide, 2,N-dicyclohexyl-2-[2·(2·ethoxy-phenyl)- Benzimidazol-1-yl]-acetic acid amine, 2-[2-(6-chloro-pyridin-3-yl)-benzimidazol-1-yl]-2, fluorene-dicyclohexyl-ethylamine, 2-[2-(2-Ga-pyridin-4-yl)-benzimidazol-1-yl]-2, fluorenyl-dicyclohexyl-ethyl 121967. Doc -24- 200811112 Amine, 2-[2-(4-gas-phenyl)-6-gas-benzoquinone ηm° sit-1-yl]-2,Ν-:ί^ hexyl-acetamide , 2, Ν-di-dihexyl-2-[2-(3- gas-4-oxo-phenyl)-benzoquinone 117 m唆-1_yl]-acetic acid amine, 2-[2-(4- Chloro-3-methyl-phenyl)-benzimidazol-1-yl]·2, fluorene-dicyclohexyl-acetamide, 2_[2-(3-chloro-2-methyl-phenyl)- Benzimidazol-1-yl]-2, fluorene-dicyclohexyl-acetamide, 2-[2-(4-chloro-3-gas-phenyl)-benzo 11 m quinone-1-yl] -2, Ν·二 哀 己 --acetamide, 2-[2-(3-chloro-4-fluoro-phenyl)·benzimidazol-1-yl]-2, fluorene-dicyclohexyl-B Guanidine, 2, fluorene-dicyclohexyl-2-[2-(5.methyl-1Η-吲哚_2-yl)-benzimidazol-1-yl]-acetamide, 2, sense ring Hexyl-2_[2-(2,3,4-trifluoro-phenyl)-benzimidazol-1-yl]-acetamide, 2, fluorene-dicyclohexyl-2-[2-(2,4 , 5-trifluoro-phenyl)-benzimidazol-1-yl]-acetamide, 2-(2-benzo[b]thiophen-2-yl-benzimidazol-1-yl)-2, Ν-dicyclohexyl-acetamide, 2, fluorene-di-dextyl- 2·[2-(5-gas-1Η-ϋ引口-2-yl)-benzoquinone m°-1 -based ]_ acetamide , 2-(2-benzothiazol-6-yl-benzimidazol-1-yl)-2, fluorene-dicyclohexyl-ethene 121967. Doc -25- 200811112 Amine, 2,N-dicyclohexyl-2-[2-(4-isopropoxy-phenyl)-benzimidazol-1-yl]-acetic acid amine, 2,N-bicyclic Hexyl-2-[2-(3,4-dimethoxy-phenyl)-benzimidazol-1-yl]-acetamide, 2,N-dicyclohexyl-2-[2-(2, 5-dimethoxy-phenyl)-benzimidazol-1-yl]-acetamide, 2,N-dicyclohexyl-2-[2-(2-difluorodecyloxy-phenyl)- Benzimidazol-1-yl]-acetamidamine, 2,^^-di-f-hexyl-2-[2-(4-dimethoxymethoxy-phenyl)-benzoquinone-1_yl]-B Indoleamine, 2,1^-diazepine-2-[2-(3-disorganomethoxy-phenyl)-benzoquinone. Sit -1_yl]-acetamide, 2, Ν·2 ί hexyl-2-[2-(4-dimethylmethyl-phenyl)-benzoquinone °°-1-yl]_acetamide , 2,N-二ϊϊ己基- 2- [2-(3,4-di-phenyl-phenyl)-benzoquinone 1^米ϋ-1-yl]-ethylamine, 2-[2-( 4-&gt;odor-phenyl)-benzo σm σ sit-1-yl]-2, Ν-diazepine-ethylamine, 2, Ν-di-dihexyl-2- [2-(6- Methoxy-naphthyl-yl)-benzoquinone-flavored σ-l-yl]-acetamide, 2, fluorene-dicyclohexyl-2-[2-(3-trifluoromethoxy-phenyl) )-benzimidazol-1-yl]-acetamide, 2, Ν-. A bad hexyl- 2- [2-(7-ethoxy-benzo-benzo-2-yl)-benzoquinone miso sitting - 121967. Doc -26- 200811112 1 -yl]-acetic acid amine, 2,N-:^-hexyl-2-[2-(3- gas-4-dimethyl-phenyl-phenyl)-benzoquinone m°-1 · ]]-acetamide, 2,N-d-hexyl-yl-[2-(6-diethylamino-σ- -3-yl)-benzoquinone σ米峻_ 1-yl]- Acetamine, 2-[2-(2-chloro-5-mercapto-phenyl)-benzimidazol-1-yl]_2, fluorene-dicyclohexyl-acetamide, 2-[2-(5 -Gas-2-methyl-phenyl)-benzoquinone.米°坐-1-基]-2,Ν-二ί哀基· acetamidine, 2-[2-(2·6-methyl-phenyl)-benzoquinone-sodium-l-based] -2, Ν-di-dihexyl·acetamide, 2, fluorene-dicyclohexyl-2-(2-quinolino-6-yl-benzimidazol-1-yl)-acetamide, 2-[ 2-(5-Gas-2-a-phenyl)-benzoquinone 1:7 m jun-1 -yl]-2,N-di-f-hexyl-acetamide, 2,N-dicyclohexyl-2- [2-(4-Methoxy-3,5-dimethyl-phenyl)-benzopyridinyl-1 -yl]-ethenylamine 2,N-dicyclohexyl-2-[2- (2,3-dimethoxy-phenyl)-benzimidazole-1-yl]-acetamide, 2-[2-(3-chloro-4-methoxy-phenyl)-benzimidazole -1-yl]-2,N-dicyclohexyl-acetamide, 2,N-dicyclohexyl-2-[2-(2,5-dichloro-phenyl)-benzimidazol-1-yl ]-acetamide, 2-[2-(3-chloro-2,4-difluoro-phenyl)-benzimidazol-1-yl]-2,N-dicyclohexyl-27- 121967. Doc 200811112 base-acetamide, 2-[2-(2_chloro-4,5-difluoro-benyl)-benzoxanthene-1_yl]_2,^^-dicyclohexyl-acetamide , 2,N-Dicyclohexyl-2-[2-(4-diethylamino-phenyl)- benzoimidazole β1_yl]-acetamide, 2-[2-(4-benzylidene) -phenyl)-benzo-indol-1-yl]-2,]^dicyclohexyl-acetamide, (S)-2-[2-(4-cyano-phenyl)-benzo. Rice n-yl]_2,N-dicyclohexyl-acetamide, 2,N-dicyclohexyl-2-[2-(4-phenoxy-phenyl)-benzimidazolyldiethylamine, 2,;^_Dicyclohexyl-2-[2-(2-phenoxy-phenyl)-benzimidazole-buyl]-acetamide, 2,N-dicyclohexyl-2-[2- (3-phenoxy-phenyl)-benzimidazole·^ benzylamine, 2,N-dicyclohexyl-2_{2-[2-(1,1,2,2_tetrafluoro-B Oxyphenyl)-phenyl]-benzimidazol-1-yl}•acetamidine, 2,N-dicyclohexyl-2-{2-[3-(1,1,2,2-tetrafluoro-B Oxy)phenyl]-benzimidazole-l-yl}-acetamide, 2,yicyclohexyl-2_{2_[4-(1,1,2,2-tetrafluoro-ethoxy) _Phenyl]-benzo-salt-salt-1-yl}-acetamide, 2,N-dicyclohexyl-2-[2-(4.-trifluoromethyl-biphenyl-4-yl)-benzene并口米嗤-1_基]-acetamide, 2,&gt;^-dicyclohexyl-2-[2-(3',4'-di-benzene-4-yl)-benzimidazole-1 - 121967. Doc •28- 200811112 base]-acetamide, 2,N-dicyclohexyl-2-[2_(2,4-dichloro-5-aminesulfonylphenyl)benzoimidazole-1-yl ]-acetamide, (S)-2-[6-gas-2-(4- gas-phenyl)-5-gas-benzoquinone-s-l-yl]-2,N-di 哀 己-acetamide, 2, Ν·dicyclohexyl-2-(2-pyridin-2-yl-benzimidazol-1-yl)-acetamide, 2,N-dicyclohexyl-2-[2- (6-methyl-acridin-3-yl)-benzimidazole-l-yl]-acetamide, 2,N-dioxasyl- 2- [2-(3-methyl-π ratio σ -2--2-yl)-benzoquinone misoquinone-1 -yl]_acetamide, 2, fluorene-dicyclohexyl-2- [2-(6-methyl-° ratio σ-but-2-yl) ) - Benzo flavor. Sodium-1 -yl]-acetamide, 2-[2-(2-amino-11-buty-3-yl)-benzoquinone-flavor-1-yl]-2, fluorene-bis-hexyl-based Amine acetate, 2_[2-(6-cyano-acridin-3-yl)-benzimidazol-1-yl]·2, fluorenyl-dicyclohexyl-acetamide, 2, fluorene-di- hexyl- 2-[2-(2·methyllacyl-0-pyridin-3-yl)-benzophenanthrene quinone-1 _yl]-acetamide, 2-[2-(2- gas-6-A Base - ° ratio σ -3 - yl) - phenyl hydrazine - 1 - yl] - 2, Ν · di- hexane-acetamide, 2-[2-(2- gas-6-methyl-啶-4-yl)-benzimidazol-1-yl]-2, fluorene-dicyclohexyl-acetamide, 2, fluorene-di-dihexyl-2 - (2 · wow' scare ^ - 3 - group - benzoquinone taste. sit -1 - base) - ethyl amine '2, Ν - two bad hexyl-2 - (2 - 喧 ^ ^ - 4 - base · benzoquinone taste π sit -1 - base) - Amine ' 121967. Doc -29- 200811112 2-[2-(3-Gas-4-difluoromethyl-phenyl)_ benzo oxime _1 hexyl-acetamide, yl]-2, t-bicyclic (S)- 2-[2-(4-Chloro-phenyl)-benzophenanthrene. Sitting on a small base]·4 guanamine, earth pentacycline cyclohexyl 2-(4•gas-phenyl)-2-[2_(heart phenyl)_benzoxazolyl·acetamide, cyclohexane 2- [2-(4-Chloro-phenyl)-benzimidazole _ 丨-yl]cyclohexyl-phenyl)-acetamide, soil difluoromethyl 2-[2-(4·g·phenyl)-benzene And imidazole "- kibu...cyclohexyl j ^ phenyl)-acetamide, soil 3,4 · dichloro -2- [2-(4- gas-phenyl) benzophenanyl) -acetamide, hexyl-based external methoxy group - 2 cases of 4-gas-phenyl)-benzo(tetra)]-yl]_N_cyclohexylacetamide, TT base _ 2-[2-(4-chloro -phenyl&gt;benzimidazole-;1-yl)-acetamide, hexyl, 3-fluorobenzene 2-[2-(4•gasphenyl)-benzo(tetra)cyclohexyloxy-phenyl )-acetamide, v Τ 2-[2-(4·chloro-phenyl)-benzoiminyl]_ν_cyclohexylphenyl)-acetamide, (5-mono-no-chloro) -phenyl)·benzoxazole small group]·ν_cyclohexyloxy-phenyl)-acetamide, 1 gas·5-methyl(s)-2-[2-(5mphenyl)-benzene And the body 丨 _ keto-amine, one percent has been 121967. Doc -30 - 200811112 (S)-2,N·Dicyclohexyl_2_[2_(2,3-dimethoxyphenyl)_benzoic.  Base]-Ethylamine, (S) 2 [2 (3-chloro-4-methoxy-phenyl)-benzopyrene 2 dicyclohexyl-acetamide, ' , (8) stomach 2 · ring Hexyl·2_[2·(2,4·dimethoxyphenyl)-benzo-N-(2,6-dimethyl-phenyl)-acetamide, 2-[2-(4- Chloro-phenyl)-benzophenidate σ sitting on a small base]·2_cyclohexyl-Qin(4,xindiqi_cyclohexyl)-acetamide, (S)-2-[2-(4-chloro-benzene (B)-Benzimidazolyl]_2_cyclohexyl_^_(4,4_digas- 哀 己 基)-Ethylamine '(8)-2-[2-(2-Amino-吼 bite~ 3_基)-Benzimidine σ sit; [基]_2,Ν•Dicyclohexyl-ethonamine ' 2,Ν-dicyclohexyl-2-(6-fluoro-2-pyridine_2-yl) Benzimidazolyl)-acetamide, 2,N-dicyclohexyl-2-[2-(2,4-dimethoxy-phenyl)-6•fluoro-benzimidazole _ 1-yl]-B Indoleamine, 2, Ν·dicyclohexyl-2-[6-fluoro-2-(4-methoxy-phenyl)-benzoxazole·^yl]-acetamide, 2, fluorene-one哀 己 基 _2 - - _2 _2 _2 _2 _2 _2 _2 _2 _2 _2 2- 2- 2- 2- 2- 2- 2- 2- 2- 2- 2- 2- 2- 2- 2- 2- 2- 2- 2- 2- 2- 2- 2- 2- 2- 2- 2- 2- 2- 2- 2- 2- 2- 2- 2- 2- 2- 2- 2- 2- 2- 2- 2- 2- 2- 2- 2- 2- 2- 2- 2- 2- 2- 2- 2- 2- 2- 2- 2- 2- 2- 2- 2- 2- 2- 2- 2,3-dimethoxy-phenyl)-6-fluoro-benzoxazole·1-yl]-acetamide, 2,N-dicyclohexyl-2-[2-(2 -ethyl-5-methyl-2H-pyrazole-3-yl)-6-oxybenzimidazol-1-yl]-acetamide, 121967. Doc -31 - 200811112 2,1^-di-dextyl-2-[2-(3,5-dimethyliso-oxo.spin-4-yl)-6-gas-benzimidazol-1-yl] -acetamide, 2,N-dicyclohexyl-2-[6-fluoro-2-(1Η-oxazol-4-yl)-benzimidazol-1-yl]-acetamide, 2,N- Dicyclohexyl-2-[2-(l,5-dimethyl-1H-.pyrazol-3-yl)-6-fluoro-benzimidazol-1-yl]-acetamide, 2,N-二ί莉基基-2-[6-乱乱-2-(3 -Methyl-iso- σ°°-5-yl)-phenylhydrazin-1-azole]-acetamide, 2, Ν- Dicyclohexyl-2·[6-fluoro-2-(lHパpyrrol-2-yl)-benzimidazole-1-yl]-acetamide, 2, fluorene-dicyclohexyl-2-[6- Gas- 2·(3-methyl-σ-shen-2-yl)-benzoquinone 17-spin-1-yl; acetamidine, hydrazine-benzyl-2-[2-(4-chloro-benzene) -benzimidazol-1-yl]-2-cyclohexyl-acetamide, N-butyl-2-[2-(4-chloro-phenyl)-benzimidazol-1-yl]-2 -cyclohexyl-acetamide, 2-[2-(4-chloro-phenyl)-benzimidazol-1-yl]-N-cyclohexyl-2-(tetrahydro-pyran-4-yl)- Ethylamine '2-[5-chloro-2-(4-chloro-phenyl)_6.fluoro-benzimidazol-1-yl]-2,N-dicyclohexyl-acetamide, 2-[2 -(4-chloro-phenyl)-5,6-difluoro-benzimidazole-1 -yl]·2, Ν-dicyclohexyl-acetamide, 2-[2-(4- gas·phenyl)-benzo.米°坐-1-基]-2 - 哀哀己基-Ν-(四鼠-派 -4-yl)-acetamide, 121967. Doc -32- 200811112 2-[2-(4-Chlorophenyl)-benzimidazol-1-yl]-2-cyclohexyl-N-cyclopropyl-acetamide, 2,N-dicyclohexyl -2-[2-(6-morpholin-4-yl-pyridin-3-yl)-benzimidazol-1-yl]-acetamide, (S)-2-[2-(4-chloro- Phenyl)-benzimidazol-1-yl]-2-cyclohexyl(tetrahydro-pyran-4-yl)-ethanoamine '(S)-2,N-dicyclohexyl-2-[2- (4-decanesulfonyl-phenyl)-benzimidazolyl-1-yl]-ethonamine '(S)-2-[2-(4-chloro-phenyl)-benzimidazole-1- 2-cyclohexyl-N-cyclopropyl-acetamide, 2-[6-Gas-2-(4-chloro-phenyl)-5-fluoro-benzimidazol-1-yl]-N -cyclohexyl-2-(tetra-m-amyl-4-yl)-ethonamine '(S)-2-[2-(4-chloro-phenyl)-benzimidazol-1-yl]-N -cyclohexyl-2·(tetrahydro-pyran-4-yl)-ethonamide '(S)-2-[6-chloro-2-(4-chloro-phenyl)-5-fluoro-benzo Imidazolyl-1-yl]-N-cyclohexyl-2 _ (tetrazo-bran-4-yl)-ethylamine '(S)_2-[2-(4·chloro-phenyl)-5,6 -difluoro-benzimidazol-1-yl]-2,N-dicyclohexyl-acetamide, (S)-2-[2-(5-chloro-thiophen-2-yl)-benzimidazole- 1-yl]-2,N-dicyclohexyl-acetamide, (S)-2,N-dicyclohexyl-2-[2-(2,3- Difluoro-phenyl)-6-fluoro-benzimidazole-1-yl]-acetamide, 2-[6-chloro-2-(4-chloro-phenyl)-5-qi-benzoquinone. Sodium-1-yl]-N-lycopeptyl-2_cyclopentyl-acetamide, 121967. Doc -33- 200811112 (S)-2-[6-Chloro-2-(4-chloro-phenyl)-5-indole-benzoquinone-methyl-1-yl]-heptanoic acid S)-2-[6-Chloro-2-(4-carb-phenyl)-5-fluoro-benzimidazol-1-yl]-indole-cyclohexyl-2-azain-ethylamine-2 -[2-(4-chloro-phenyl)-5-fluoro-benzimidazol-1-yl]-2,N-dicyclohexyl-acetamide, 2-[1-(cyclohexyl-cyclohexylamine) Methylmercapto-methyl)-5,6-difluoro-1H-benzoimidazol-2-yl]-benzoic acid methyl ester, 2,N-dicyclohexyl-2 - (5,6-digas-2 -ϋ ratio 17 定·2 -yl-benzoquinone m ^s-1 -yl)-acetamide, 2-[2-(5-chloro-indol-2-yl)-5,6-difluoro -benzoic acid °-1-yl]-2, fluorene-dicyclohexyl-acetamide, 2-[6-chloro-1-(cyclohexyl-cyclohexylaminemethyl fluorenyl-methyl)-5- Fluorine-111-benzimidazol-2-yl]-benzoic acid methyl ester, 2-(6-chloro-5-fluoro-2-tonidin-2-yl-benzimidazole-1.yl)·2,Ν -dicyclohexyl-acetamide, 2-(6-chloro-5-fluoro-2-pyridin-3-yl-benzimidazol-1-yl)-2, fluorene-dicyclohexyl-acetic acid amine, 2- (6-chloro-5-fluoro-2-pyridin-4-yl-benzimidazole-1·yl)-2,indole-dicyclohexyl-acetamide, 2-[6-chloro-2-(3- Gas-thiophen-2-yl)-5- -benzimidazol-1-yl]-2,anthracene dicyclohexyl-acetamide, 2_[6-chloro-2-(5-a-thiophen-2-yl)-5-fluoro-benzimidazole- 1-yl]-2, fluorene dicyclohexyl-acetamide, 121967. Doc -34- 200811112 (S)-2-[6-Gas-2-(4-Ga-phenyl)_5_Fluoro-benzoxanthene+yl]Winterethyl-pentanoic acid cyclohexylamine, 2- [6-Gas_5-Gas-2-(4-Fluoro-phenyl)-benzo-b-butyrazole-1-yl]_2,yi-dicyclohexyl-ethylamine, 2-[2-(4-chloro- Phenyl)-benzo-salt-small base]·2_cyclohexyl good (1) isopropyl-2·methyl-propyl)-ethylamine, 2-[6-order 2-(4-chloro-phenyl) -5 Benzene and rice. Sitting on a small base]_2_cyclohexyl-s-cyclopentyl-acetamide, 2-[2 as chloro-phenyl)_5,6·difluoro-benzoiminyl]·n_cyclohexyl·2_ (tetrahydrogen) -piperidin-4-yl)-acetamide, (S)-2-[2-(4j-phenyl)_5_fluoro_ benzoheptazole small base 2, Ν_dicyclohexyl-ethonamide , 2^4-gas-phenyl)_5,6_diox·benzimidazole-diyl]_2_cyclohexyl (tetrahydro-l-butan-4-yl)-acetamide, chloro-2- (4-Chloro-phenyl)_5_fluoro-benzopyranyl]_2_cyclohexyl (tetrahydro-bran-4-yl)-acetamide, 2'Ν-dicyclohexyl_2_[ 2-(3-dimethylamino-phenyl)-5,6-diimidazol-1-yl]-acetamide, the present 2, Ν--% hexyl-2- [2-(3-dimethyl) The base of the face is poor, γ ^ 1-yl] • acetamidine, W-based gas - stupid and ^ phenyl) -5,6 · difluorobenzimizol-1 ·yl]_2-cyclohexyl* (1-isopropyl-2-methyl-propyl)-acetamidamine, 2-[6-Gas-2-(4-chloro-phenyl)_5-fluorobenzimidazole-based 2-ring Hexyl (1-isopropyl-2-methyl-propyl)-acetamide, Yitu-Ν- 121967. Doc -35- 200811112 2-[2-(3-Chloro-phenyl)-5,6-difluoro-benzimidazol-1-yl]-2,N-dicyclohexyl-acetamide, 2-[ 2-(2-Gas-phenyl)-5,6-difluoro-benzoimidazol-1-yl]-2,N-dicyclohexyl-acetamide, (S)-2-[6-chloro- 5-Qi-2-(4- gas-phenyl)-benzoquinone-salt-l-yl]-2,N-dioxayl-acetamide, (S)-2-[2-(4- Chloro-phenyl)-5,6·difluoro-benzimidazol-1-yl]·Ν-cyclohexyl- 2- (tetrachloro-branol-4-yl)-ethonamine 2- 2- (4-Chloro-phenyl)-5-fluoro-benzoimidazol-1-yl]-N-cyclohexyl-2-(tetrahydro-pyran-4-yl)-acetamide, 2-[2_( 4-Chloro-phenyl)-6-fluoro-benzoimidazol-1-yl]-N-cyclohexyl-2-(tetrazine-l-amyl-4-yl)-ethanoamine '2-[2-( 4-chloro-phenyl)-6-say-benzoate °-1-yl]-N-defenyl-2-(tetrazine-bungan-2-yl)-acetone-amine 2-[6 -Chloro-2-(4-chloro-phenyl)-5-f-benzophenone-flavored σ-l-yl]-N-cyclohexyl- 2-(four-money-bran-2-yl)-ethyl Amine '(S)-2,N-dicyclohexyl-2-[6-gas-2-(3-methyl·σ塞-2-)-phenylhydrazin-1-yl]-B Indoleamine, (S)-2-[2-(2-chloro-phenyl)-5,6-difluoro-benzimidazol-1-yl]-2, hydrazine -dicyclohexyl-acetamide, (S)-2-[2-(4-chloro-phenyl)-5-fluoro-benzimidazol-1-yl]-indole-cyclohexyl-2-(tetrahydro) - britium-4-yl)-acetamide, (S)-2-[2-(4-chloro-phenyl)-6-gas-benzoquinone 17 m唆-l-yl]-N-lycopene -2_ (Four Rats - Brigade-4 -Base) - Ethylamine ' 121967. Doc •36- 200811112 (S)-2-[2-(4·Chloro-phenyl)-6-fluoro-benzimidazol-1-yl]-N-cyclohexyl-2·(R)-tetrazine-鲁尔-2-yl-ethyl-amine '(S) -2-[2-(4-chloro-phenyl)-6-fluoro-benzimidazol-1-yl]-indole-cyclohexyl-2-( S)-Four squirrel-2-yl-ethylamine, 2-[2-(4-chloro-phenyl)-5-fluoro-benzimidazol-1-yl]-N-cyclohexyl-2- (tetrazole-bungan-2-yl)-ethonamide '2^-diclofenyl-2-[2-(3,4-di-phenyl)-6-indole-phenylhydrazine 17 m 11 sit-1 -yl]-ethylamine ' 2 ·[2-(4-Gas-phenyl)-6-methoxy-benzimidazol-1-yl]-2,N-dicyclohexyl-B Indoleamine, 2-[2-(5-chloro-thiophen-2-yl)-6-methoxy-benzimidazol-1-yl]-2,N-dicyclohexyl-acetamide, 2-[ 2-(3-Chloro-4-methoxy-phenyl)-6-methoxybenzimidazol-1-yl]-2,N-dicyclohexyl-acetamide, 2-[2-( 4-ox-3-fluoro-phenyl)-6-decyloxy-benzimidazol-1-yl]-2,N-dicyclohexyl-acetamide, 2-cyclohexyl-N- sulphonyl- 2-[2-(3,4-dioxa-phenyl)-6-methoxy-benzimidazole-1 yl]-acetamide, N-cyclohexyl-2-cyclopentyl-2-[ 2-(3,4-dioxa-phenyl)-6-methoxy-benzimidazol-1-yl]-B Amine, 2-[2-(4-chloro-phenyl)-6-methoxy-benzoimidazol-1-yl]-2-cyclohexyl-N-cyclopentyl-acetamide, 2-[2 -(3- gas-phenyl)-6-hydrazinyl-benzoquinone σ m. Sit · 1 -yl]-2,N-dioxahexyl-acetamide, 121967. Doc -37- 200811112 2,^^-di-decyl-2-(2-(3,4-di-phenyl)-6-methoxy-benzoquinone miso-1-1-yl]-acetamidine Amine, 2-[2-(4- gas-phenyl)-6-methoxy-benzoquinone-flavor-1-yl]N-defenyl-2_cyclopentyl-acetamide, 2-[ 2-(4- gas-3-ran-phenyl)-6-methoxy-benzoquinone 11 m ϋ-1-yl]-2-3⁄4 hexyl-N-cyclopentyl-acetamide, 2- [2-(3- gas-4-methoxy-phenyl)-6·曱-milyl-benzoquinone 0 m sal-l-yl]-2_ 玉哀己基_ N- sulphonyl-ethonamide 2,N-dioxahexyl-2-[2-(4-mur-phenyl)-6-methoxyi-benzoyl salic-1 _yl]-acetamide, 2-[2-( 3-Gas-phenyl)-6-methoxy-benzoquinone. -1--1-yl]-2-3⁄4 hexyl-N-cyclopentyl-acetamide, 2-[2-(3- gas-4-methoxy-phenyl)-6-methoxy-benzo-1 :7 m唆-1 -yl]-N_cyclohexyl-2-cyclopentyl-acetamide, 2-[2-(5-gas-σ-sec-2-yl)-6-methoxy-benzene Astringent σ sit-1-yl]-N-lymphenyl-2-cyclopentyl-acetamide, 2-cyclobutyl-indole-cyclohexyl-2- [2-(3,4-digas-benzene) -6-methoxy-benzimidazol-1-yl]-acetamide, 2-[2-(5-gas-σ-secen-2-yl)-6-methyllacyl-benzoate ° sit-1-yl]-2-3⁄4 hexyl-N- 哀 戊 基 - 乙 2- 2- 2- 2- 2- 2- 2- 2- 2- 2- 2- 2- 2- 2- 2- 2- 2- 2- 2- 2- 2- 2- 2- 2- 2- 2- 2- 2- 2- 2- 2- 2- 2- 2- 2- 2- 2- 2- 2- 2- 2- 2- 2- 2- 2- 2- 2- 2- 2- 2- 2- 2- 2- 2- 2- 2- 2- 2- 2- 2- 2- 2- 2- 2- Benzene mouth rice 11 sitting -1 -yl]·2, Ν-dicyclohexyl-acetamide, 2-[2-(3- gas-phenyl)-6-methyllacyl-benzoquinone σ sitting- 1-based]-indole-dextrinyl-2·cyclopentyl-acetamide, 121967. Doc • 38 - 200811112 2-[2-(3-Gas-4-methoxy-phenyl)-6-methoxy-benzimidazole small group] 2,N-dicyclopentyl-acetamide, 2,N-monocyclohexyl-2-[6-methoxy-2-(6-trifluoromethyl-η than 唆_3_yl)·benzimidazol-1-yl]-acetamide, 2- [2-(5-Chloro-thiophene-2-yl)-6-methoxy-benzimidazole 丨 基 基 • • • • 2- 2- 2- 2- 2- 2- 2- 2- 2- 2- - gas-phenyl)-6-methoxy-benzimidazole-yl]cyclobutyl_Ν_cyclohexyl-acetamide, and Ν-cyclohexyl-2-cyclopentyl-2_[2-(4 -Fluoro-phenyl)-6-methoxy-benzimidazol-1-yl]-acetamide, and pharmaceutically acceptable salts and esters thereof. 28. The compound according to claim 1 or 2, which is selected from the group consisting of the following: 2-[1-(cyclohexyl-cyclohexylaminecarbamyl-methyl) "ugly-benzimidazole_2-yl] · Benzamide, (S)-2,N-dicyclohexyl-2_[2-(2,4-dimethoxy-phenyl)-benzimidazolyl]-acetamide, (S)- 2_[2-(4-Chloro-phenyl)·benzotrimazole small base]_2,n-dicyclohexyl·ethylamine, (8)-2-[2-(4-chloro-phenyl)- Benzimidazole-1_yl]_4_methyl-pentanoic acid ring amide, trifluoromethyl 2-[2-(4-carbo-phenyl)-benzimidazole-1-yl]cyclohexyl- Phenyl)-acetamide, (S)-2-cyclohexyl-2-[2-(2,4-dimethoxy-phenyl)-benzimidazole _丨·美]#-(2,6 -Dimethyl-phenyl)-acetamide, soil 121967. Doc -39- 200811112 (S)-2-[2-(4-Chloro-phenyl)-benzimidazol-1-yl]-2-cyclohexyl-, (4,4-difluoro-cyclohexyl)- Acetamine, (S)-2-[6-chloro-2-(4-carbo-phenyl)-5-fluoro-benzimidazol-1-yl]cyclohexyl-2 -(tetrazole-nivine- 4-(yl)-ethonamine '(S)-2-[2-(5-chloro-thiophen-2-yl)-benzimidazol-1-yl]-2,7V-dicyclohexyl-acetamide , (S)-2-[6-Gas-2-(4-Ga-phenyl)-5-disorder-benzoquinone-flavored σ-l-yl]-heptanoic acid 哀 醯 醯 醯, 2-[6 -Gas-2-(4-Ga-phenyl)-5-fluoro-benzimidazol-1-yl]·2·cyclohexyl-, (tetraz-halo-4)yl-ethanoamine 2 -[2-(3-Gas-phenyl)-5,6-difluoro-benzimidazol-1-yl]-2,7V-dicyclohexyl-acetamide, (S)-2,N-di Cyclohexyl-2-[6-fluoro-2-(3-methyl-thiophen-2-yl)-benzimidazol-1-yl]-acetamide, (S)-2-[2-(2- Gas · phenyl) · 5,6-diqi-benzo-flavor σ-l-yl]-2,]^- diatomyl-acetamide, (S)-2-[2-(4-chloro -phenyl)-6-fluoro-benzimidazol-1-yl]-indole-cyclohexyl-2-(R)-tetrazine-nivine ►pyran-2-yl-ethanoamine '(S)-2- [2-(4-Chloro-phenyl)-6-gas-benzoquinone 11 -1-yl]-N-lymphoterol-2-(S)_tetrazole-Brigan-2- -Ethylamine 'and 2-[2-(4- gas-phenyl)-5-gas-benzoquinone °°-1-yl]-N- 哀 己 基 -2- (tetrazo- σ 辰-2 -yl)-ethonamide' and its pharmaceutically acceptable salts and esters. 29.  - A method of making a compound of formula (I) according to any one of claims 1-28, 121967. Doc -40- 200811112 This method involves cyclizing a compound of formula (Π) (II) R6, R7 and R8 are as claimed in item i_28, which is defined by the method of claim 29, wherein any one of R1, R3, r4, r5 is defined. 30. 31. 32. 33. 34. 35. In the case of the compound of claim 1 or 2, a pharmaceutical composition comprising a person as claimed in claim K28 and a pharmaceutically acceptable carrier And / or adjuvant. A compound such as Kiss 1 or 2 which is used as a therapeutically active substance. A compound according to claim 1 or 2 for use as a therapeutically active substance for the treatment and/or prevention of a disease modulated by an FXR agonist. The use of a compound according to any one of the preceding claims, which is for the preparation of a medicament for the therapeutic and/or prophylactic treatment of a disease modulated by an FXR agonist. Use of a compound according to any one of the invention for the preparation of a medicament for the therapeutic and/or prophylactic treatment of an increase in lipid and cholesterol, high LDL-cholesterol, high triglyceride, low HDL-cholesterol, lipid Abnormalities, atherosclerosis, diabetes, non-insulin-dependent diabetes mellitus, metabolic syndrome, cholesterol gallstones, cholestasis/liver fibrosis, cholesterol absorption disease, cancer, gastrointestinal 121967.doc -41 - 200811112 Cancer, osteoporosis Symptoms, peripheral obstructive diseases, ischemic stroke, Parkinsons disease and/or Alzheimer's disease 〇121967.doc -42- 200811112 VII. Designated representative map: (1) The representative representative figure of this case is: (none) (2) The symbol of the symbol of the representative figure is simple: 8. If there is a chemical formula in this case, please reveal the best indication of the characteristics of the invention. Type: 121967.doc -6-